| + |
AKT1 | down-regulates activity 
phosphorylation
|
AR |
0.605 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-108504 |
Ser215 |
SGRAREAsGAPTSSK |
Chlorocebus aethiops |
COS-1 Cell |
| pmid |
sentence |
| 11404460 |
Akt suppresses androgen-induced apoptosis by phosphorylating and inhibiting androgen receptor. Here, we demonstrate that akt phosphorylates the androgen receptor (ar) at ser-210 and ser-790 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-108508 |
Ser792 |
CVRMRHLsQEFGWLQ |
Chlorocebus aethiops |
COS-1 Cell |
| pmid |
sentence |
| 11404460 |
Akt suppresses androgen-induced apoptosis by phosphorylating and inhibiting androgen receptor. Here, we demonstrate that akt phosphorylates the androgen receptor (ar) at ser-210 and ser-790 |
|
| Publications: |
2 |
Organism: |
Chlorocebus Aethiops |
| + |
AKT | down-regulates
phosphorylation
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244140 |
Ser215 |
SGRAREAsGAPTSSK |
Homo sapiens |
Neuron |
| pmid |
sentence |
| 17470458 |
The work presented here is the first demonstration that phosphorylation at s215 and s792 by akt regulates ligand binding, and the subcellular distribution of the receptor |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
AKT1 | down-regulates
phosphorylation
|
AR |
0.605 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-154631 |
Ser215 |
SGRAREAsGAPTSSK |
Homo sapiens |
Neuron |
| pmid |
sentence |
| 17470458 |
The work presented here is the first demonstration that phosphorylation at s215 and s792 by akt regulates ligand binding, and the subcellular distribution of the receptor |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
CyclinD3/CDK11A | down-regulates quantity by destabilization
phosphorylation
|
AR |
0.507 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-273125 |
Ser310 |
TEDTAEYsPFKGGYT |
Chlorocebus aethiops |
|
| pmid |
sentence |
| 17698582 |
We found that AR was phosphorylated at Ser-308 by cyclin D3/CDK11p58 in vitro and in vivo, leading to the repressed activity of AR transcriptional activation unit 1 (TAU1). |
|
| Publications: |
1 |
Organism: |
Chlorocebus Aethiops |
| + |
CyclinD3/CDK11B | down-regulates quantity by destabilization
phosphorylation
|
AR |
0.582 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-273130 |
Ser310 |
TEDTAEYsPFKGGYT |
Chlorocebus aethiops |
|
| pmid |
sentence |
| 17698582 |
We found that AR was phosphorylated at Ser-308 by cyclin D3/CDK11p58 in vitro and in vivo, leading to the repressed activity of AR transcriptional activation unit 1 (TAU1). |
|
| Publications: |
1 |
Organism: |
Chlorocebus Aethiops |
| + |
ERK1/2 | down-regulates
phosphorylation
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244606 |
Ser516 |
VSRVPYPsPTCVKSE |
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 18511414 |
Map kinase-dependent phosphorylation at ar ser-515 was supported by the decrease in intensity of the slower migrating 23-kda band after treatment with both egf and increasing concentrations of the map kinase inhibitor, u0126 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
CDK7 | down-regulates
phosphorylation
|
AR |
0.384 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-170599 |
Ser516 |
VSRVPYPsPTCVKSE |
Homo sapiens |
|
| pmid |
sentence |
| 21157430 |
Here, we show that the transcription factor tfiih, via its cdk7 kinase, phosphorylates the androgen receptor (ar) at position ar/s515. Strikingly, this phosphorylation is a key step for an accurate transactivation that includes the cyclic recruitment of the transcription machinery, the mdm2 e3 ligase, the subsequent ubiquitination of ar at the promoter of target genes and its degradation by the proteasome machinery |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
TFIIH | down-regulates
phosphorylation
|
AR |
0.324 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-269331 |
Ser516 |
VSRVPYPsPTCVKSE |
Homo sapiens |
|
| pmid |
sentence |
| 21157430 |
Here, we show that the transcription factor tfiih, via its cdk7 kinase, phosphorylates the androgen receptor (ar) at position ar/s515. Strikingly, this phosphorylation is a key step for an accurate transactivation that includes the cyclic recruitment of the transcription machinery, the mdm2 e3 ligase, the subsequent ubiquitination of ar at the promoter of target genes and its degradation by the proteasome machinery |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAPK1 | down-regulates
phosphorylation
|
AR |
0.526 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-178718 |
Ser516 |
VSRVPYPsPTCVKSE |
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 18511414 |
Map kinase-dependent phosphorylation at ar ser-515 was supported by the decrease in intensity of the slower migrating 23-kda band after treatment with both egf and increasing concentrations of the map kinase inhibitor, u0126 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AKT | down-regulates activity
phosphorylation
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244136 |
Ser792 |
CVRMRHLsQEFGWLQ |
Chlorocebus aethiops |
COS-1 Cell |
| pmid |
sentence |
| 11404460 |
Akt suppresses androgen-induced apoptosis by phosphorylating and inhibiting androgen receptor. Here, we demonstrate that akt phosphorylates the androgen receptor (ar) at ser-210 and ser-790 |
|
| Publications: |
1 |
Organism: |
Chlorocebus Aethiops |
| Pathways: | Prostate Cancer |
| + |
PP2Ca_R1A_Bd | down-regulates activity
dephosphorylation
|
AR |
0.301 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254759 |
Ser83 |
QQQQQETsPRQQQQQ |
Homo sapiens |
|
| pmid |
sentence |
| 27858941 |
DAB2IP acts as a scaffold protein for PP2A to suppress DHT-elicited S81 phosphorylation of the AR, preventing its nuclear translocation and binding to androgen response elements. In addition, DAB2IP can compete with the AR for binding to c-Src, thus blocking the non-genomic AR pathway |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
CDK5 | up-regulates 
phosphorylation
|
AR |
0.381 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-175696 |
Ser83 |
QQQQQETsPRQQQQQ |
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 21799006 |
Cdk5 enables phosphorylation of ar at ser-81 site through direct biochemical interaction and, therefore, results in the stabilization of ar proteins |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PTEN | up-regulates activity 
dephosphorylation
|
AR |
0.599 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277077 |
Ser83 |
QQQQQETsPRQQQQQ |
Homo sapiens |
|
| pmid |
sentence |
| 24480624 |
Furthermore, PTEN depletion increased AR protein instability, and this effect was further enhanced by p300 silencing in LAPC4 cells .|Our data demonstrate that loss of PTEN increases AR phosphorylation at Ser81 and that Ser81 phosphorylation acts as a molecular beacon that is required for the binding of p300, a key event that subsequently leads to AR acetylation, inhibition of AR ubiquitination and AR stabilization (XREF_FIG). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
CDK1 | up-regulates
phosphorylation
|
AR |
0.547 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-175692 |
Ser83 |
QQQQQETsPRQQQQQ |
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 21799006 |
At first, the data show that cdk5 enables phosphorylation of ar at ser-81 site through direct biochemical interaction and, therefore, results in the stabilization of ar proteins although ar was reported as substrates for cdk9 (5) as well as cdk1 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FER | up-regulates
phosphorylation
|
AR |
0.262 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-194749 |
Tyr225 |
PTSSKDNyLGGTSTI |
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 23906537 |
Fer is required for il-6 mediated ar activation by phosphorylating ar tyrosine 223 and binding via its sh2 domain. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
perfluorooctane-1-sulfonic acid | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268767 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
NCOA2 | up-regulates activity
binding
|
AR |
0.898 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251530 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 24239470 |
The NCOA2 gene encodes a transcriptional coactivator (SRC-2) that modulates gene expression by hormone receptors, including AR. NCOA2 is both amplified and rarely mutated in prostate cancers, with higher NCOA2 levels resulting in increased androgen signaling readout. Furthermore, as mentioned previously, SRC-3, a close homolog encoded by NCOA3, is a substrate of SPOP whose protein levels are increased by SPOP mutation, potentially linking these common point mutations to the androgen axis |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251531 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 24239470 |
The NCOA2 gene encodes a transcriptional coactivator (SRC-2) that modulates gene expression by hormone receptors, including AR. NCOA2 is both amplified and rarely mutated in prostate cancers, with higher NCOA2 levels resulting in increased androgen signaling readout. Furthermore, as mentioned previously, SRC-3, a close homolog encoded by NCOA3, is a substrate of SPOP whose protein levels are increased by SPOP mutation, potentially linking these common point mutations to the androgen axis |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
AR | up-regulates activity
binding
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251537 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
The unliganded AR resides predominately in the cytoplasm as a heteromeric complex with hsp90 and other chaperone proteins. These chaperone proteins maintain AR in a form that is receptive to ligand binding. Regulation of gene expression by androgen-activated AR occurs through receptor nuclear translocation, dimerization, and binding to androgen response elements (AREs) in the DNA of target genes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
enzalutamide | down-regulates
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-194325 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates
binding
|
NR5A1 |
0.418 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-109996 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11518799 |
Ar suppresses transcription of the lhbeta subunit by interacting with steroidogenic factor-1. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
NCOR2 | down-regulates
acetylation
|
AR |
0.579 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-101286 |
|
|
Homo sapiens |
Breast Cancer Cell, Prostate Gland Cancer Cell |
| pmid |
sentence |
| 12771131 |
In this study we assessed the effect of smrt and dax-1 on ar and pr activity in the presence of both agonists and partial antagonists. We show that smrt and dax-1 repress agonist-dependent activity of both receptors, and the mechanism of repression includes disruption of the receptor dimer interactions rather than recruitment of histone deacetylases. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
testosterone | up-regulates activity
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251553 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
Testosterone is the predominant circulating androgen in mammals and is converted to dihydrotestosterone (DHT) by 5α-reductase in certain tissues of the male urogenital tract, skin, and other target cells. DHT binds with highest affinity to AR and together with testosterone promotes AR transcriptional activity thereby ensuring the development and maintenance of male reproductive functions. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HSP90AB1 | up-regulates activity
binding
|
AR |
0.692 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251535 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
The unliganded AR resides predominately in the cytoplasm as a heteromeric complex with hsp90 and other chaperone proteins. These chaperone proteins maintain AR in a form that is receptive to ligand binding. Regulation of gene expression by androgen-activated AR occurs through receptor nuclear translocation, dimerization, and binding to androgen response elements (AREs) in the DNA of target genes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HOXB13 | down-regulates quantity by repression 
transcriptional regulation
|
AR |
0.509 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254475 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 15604291 |
These results suggest that HOXB13 functions as an AR repressor to modulate the complex AR signaling and subsequent growth regulation of prostate cancer cells. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
BTG1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253673 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
UCN |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253688 |
|
|
Homo sapiens |
Umbilical Vein |
| pmid |
sentence |
| 23801677 |
When cells were treated with DHT alone, AR was upregulated and translocated into the nuclei, which might repress UCN1 expression via a potential androgen-responsive element found in human CRF family promoter|These data suggest that DHT differentially influences UCN1 levels under normal and inflammatory conditions in human umbilical vein endothelial cells, which involves AR-dependent and -independent mechanisms respectively. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PHB | down-regulates quantity by repression
transcriptional regulation
|
AR |
0.462 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268977 |
|
|
|
|
| pmid |
sentence |
| 16964284 |
We now present evidence that PHB, which has 54% homology at the protein level to the oestrogen receptor corepressor REA (repressor of oestrogen receptor activity), can repress androgen receptor (AR)-mediated transcription and androgen-dependent cell growth. |
|
| Publications: |
1 |
| + |
AR | up-regulates
|
Proliferation |
0.7 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251540 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
AR homodimers recruit a panoply of factors including coactivators and mediator proteins whose enzymatic activities promote chromatin remodeling and transcriptional regulation of target genes leading to cell differentiation, survival, and proliferation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
ZMIZ1 | up-regulates activity
binding
|
AR |
0.698 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263935 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 14609956 |
Our results demonstrate that hZimp10 is a novel AR interacting protein that augments AR-mediated transcription. Moreover, hZimp10 co-localized with AR and SUMO-1 at replication foci throughout S phase, and it was capable of enhancing sumoylation of AR in vivo. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ESR1 | down-regulates quantity by repression
transcriptional regulation
|
AR |
0.425 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-82158 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11000528 |
Inhibition of ar-induced transactivation that was er cdna dose-responsive and estradiol dependent |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FOXA1 | down-regulates quantity by repression
transcriptional regulation
|
AR |
0.758 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251541 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 24875621 |
FOXA1 directly inhibits AR expression and thus the transcription of its target genes. FOXA1 inhibits AR gene expression in prostate cancer. oss of FOXA1 may lead to androgen-independent AR signaling and thus castration-resistant prostate cancer progression. Indeed, we have recently reported that FOXA1 is downregulated in CRPC |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
SERPINB5 |
0.412 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253685 |
|
|
|
|
| pmid |
sentence |
| 16304843 |
In addition, androgen receptor (AR) can recognize and bind to the ARE element, and then inhibit the activity of maspin promoter |
|
| Publications: |
1 |
| + |
GNRH1 | down-regulates activity
binding
|
AR |
0.473 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259267 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 17202804 |
GnRH antagonizes testosterone activation of the human androgen receptor in SCL60 cells. Gonadotropin-Releasing Hormone Functionally Antagonizes Testosterone Activation of the Human Androgen Receptor in Prostate Cells through Focal Adhesion Complexes Involving Hic-5 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
bisphenol A | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268732 |
|
|
in vitro |
|
| pmid |
sentence |
| 31995776 |
This study investigated the endocrine-disrupting activity of BPA, BPF, and BPS alone or as a mixture and the agonistic and antagonistic activity of the BPs using an in vitro bioassay to detect ER-, AR-, and AhR-mediated activity. Here, we evaluated the endocrine-disrupting risks of the bisphenols by investigating their agonist and antagonist activities with the estrogen (ER), androgen (AR), and aryl hydrocarbon (AhR) receptors. Our results showed that BPA, BPS, and BPF (BPs) have estrogen agonist and androgen antagonist activities and decrease the ERα protein level. . |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
STK4 | down-regulates
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-151712 |
|
|
|
|
| pmid |
sentence |
| 21512132 |
Mst1 plays a critical role in the regulation of programmed cell death and it has been implicated in PCa development. Interestingly, MST1 has been detected in AR-chromatin complexes, and forced expression of MST1 reduces AR binding to androgen-responsive elements along the PSA promoter. |
|
| Publications: |
1 |
| + |
fluoxymesterone | up-regulates activity
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259264 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10077001 |
The anabolic steroids, oxandrolone and fluoxymesterone, have high inhibition constants for binding, yet induce the N/C interaction and stabilize AR at relatively low ligand concentrations and are AR agonists in vivo. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide | down-regulates
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-190323 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
NR3C1 | down-regulates activity
binding
|
AR |
0.526 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-48516 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 9162033 |
Androgen and glucocorticoid receptor heterodimer formation. A possible mechanism for mutual inhibition of transcriptional activity. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
KDM4B | up-regulates quantity by expression
transcriptional regulation
|
AR |
0.336 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254541 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23435229 |
KDM4B enzymatic activity is required to enhance AR transcriptional activity |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
binding
|
NR3C1 |
0.526 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-48513 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 9162033 |
Androgen and glucocorticoid receptor heterodimer formation. A possible mechanism for mutual inhibition of transcriptional activity |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
CLK3 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253672 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
NRAS |
0.287 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253676 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
methyltestosterone | up-regulates activity
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259266 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 17202804 |
GnRH antagonizes testosterone activation of the human androgen receptor in SCL60 cells. Gonadotropin-Releasing Hormone Functionally Antagonizes Testosterone Activation of the Human Androgen Receptor in Prostate Cells through Focal Adhesion Complexes Involving Hic-5 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251545 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 24505269 |
Recurrent gene fusion between the androgen-regulated gene TMPRSS2 and members of the ETS transcription factor family, most commonly ERG, are present in about 50% of prostate cancer cases. Presence of this fusion gene is a critical event in the development of prostate cancer. the more aggressive phenotype that arises with the presence of TMPRSS2-ERG at least in part is caused by changes in the tumor stroma. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253686 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20308527 |
We demonstrate that CHD8 directly associates with AR and that CHD8 and AR simultaneously localize to the TMPRSS2 enhancer after androgen treatment. In the LNCaP cell line, reduction of CHD8 levels by small interfering RNA treatment severely diminishes androgen-dependent activation of the TMPRSS2 gene. We demonstrate that the recruitment of AR to the TMPRSS2 promoter in response to androgen treatment requires CHD8 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253687 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 21761340 |
The prostate-specific TMPRSS2 gene, while upregulated by AR activity in luminal cells, is also transcribed in basal populations, confirming that AR acts as an expression modulator. |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
perfluorodecanoic acid | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268770 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
NKX3-1 | down-regulates quantity by repression
transcriptional regulation
|
AR |
0.518 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251547 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16697957 |
Whereas androgen receptor (AR) positively regulates NKX3.1 expression, NKX3.1 negatively modulates AR transcription and consequently the AR-associated signaling events. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
KDM4C | up-regulates activity
binding
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263879 |
|
|
Homo sapiens |
Prostate Cancer Cell Line |
| pmid |
sentence |
| 29207681 |
JMJD2C was found to be co-localized with AR and LSD1 in the epithelium of prostate carcinoma and normal prostate cells. For the detailed mechanism, JMJD2C, AR and LSD1 assembled on the chromatin to remove the methyl groups from mono-, di- and trimethylated H3K9. Importantly, JMJD2C specifically removed the demethylation of the trimethyl H3K9 marks and modulated the transcriptional activity of AR. Moreover, JMJD2C cooperated with LSD1 and activated AR-mediated gene expression via decreasing H3K9me3 at the promoter of AR targeting genes KLK2 and PSA. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
perfluorononanoic acid | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268769 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
TRIM24 | up-regulates
binding
|
AR |
0.405 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-189113 |
|
|
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 19909775 |
We found that trim24/transcriptional intermediary factor 1alpha (tif1alpha), which is known as a ligand-dependent nuclear receptor co-regulator, interacts with ar and enhances transcriptional activity of ar |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ENOBOSARM | up-regulates
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-195892 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
nilutamide | down-regulates
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-194649 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
CYP7B1 |
0.293 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253739 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 16630558 |
DHT and overexpression of androgen receptor (AR) suppressed CYP7B1 promoter activity and CYP7B1-mediated catalysis in kidney-derived HEK293 cells. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
CDKN1A |
0.364 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253675 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
DDX5 | up-regulates
binding
|
AR |
0.326 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-181456 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18829551 |
P68 is a nuclear protein and interacts with ar / p68 co-occupies the active psa promoter at are regions and enhances ar transcriptional activity |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
EZH2 | up-regulates activity
binding
|
AR |
0.557 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251542 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23239736 |
This study demonstrates that phosphorylation of EZH2 at Ser21, mediated directly or indirectly by the PI3K-Akt pathway, can switch its function from a Polycomb repressor to a transcriptional coactivator of AR (and potentially other factors). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
NR0B2 | down-regulates
binding
|
AR |
0.425 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-112589 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11735420 |
We demonstrated that shp inhibited both ar-lbd and ntd-dependent transactivation, which evidenced for the first time a protein capable of inhibiting a steroid receptor amino-terminal-dependent transactivation. We further characterized the shp mechanism of action by showing that shp reversed ar coactivator-mediated activation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
CRH |
0.311 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268723 |
|
|
Homo sapiens |
Neuroblastoma Cell |
| pmid |
sentence |
| 16446741 |
A direct androgenic involvement in the expression of human corticotropin-releasing hormone|A potential androgen-responsive element (ARE) in the human CRH promoter was subsequently analyzed with bandshifts and cotransfections in neuroblastoma cells. In the presence of testosterone, recombinant human AR bound specifically to the CRH-ARE. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
AKR1C3 |
0.462 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253737 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 22971343 |
Both AR antagonism and androgen deprivation can upregulate AKR1C3. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
SEPTIN7 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253677 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
SCN9A |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253466 |
|
|
Mus musculus |
|
| pmid |
sentence |
| 24493753 |
In neuroblastoma ND7 cells, a nuclear interaction between the developmentally regulated transcription factor Brn-3a and AR resulted in a complex which bound to multiple elements within the promoter region of SCN9A (Nav1.7) and upregulated channel expression. |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
ERBB3 | up-regulates quantity by expression
transcriptional regulation
|
AR |
0.52 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-130443 |
|
|
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 15542423 |
Suspected erbb receptor involvement in prostate cancer originates partly from the realization that these proteins are capable of promoting the transcriptional activity of the androgen receptor (ar), her2/her3 effects on ar included effects on protein stability and stimulation of dna binding to ar target genes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PKN1 | up-regulates
phosphorylation
|
AR |
0.571 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-152762 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 17251915 |
Rho can sensitize the ar to low levels of circulating androgens by promoting the nuclear translocation of a transcriptional co-activator, fhl2 (four and a half lim domains 2), which binds ar, and by stimulating protein kinase n (pkn), which phosphorylates ar directly. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HECTD4 | down-regulates quantity by destabilization
ubiquitination
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-267148 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 32814769 |
We identified several E3 ligases as strong candidates responsible for AR and MYC protein loss as HECTD4, MYCBP2, and TRIM49. HECTD4 and MYCBP2 target AR and MYC for degradation while TRIM49 appears to promote AR and MYC stability. We have shown that these E3 ligases in turn are directly regulated by MYC. MYC in turn represses the expression of ubiquitin ligases, HECTD4 and MYCBP2 that promote AR and MYC protein degradation, further suppressing MYC and AR in a feed forward loop. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
NAT1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253684 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 17210686 |
Induction of human arylamine N-acetyltransferase type I by androgens in human prostate cancer cells|We show that NAT1 activity is induced by R1881 in androgen receptor (AR)-positive prostate lines 22Rv1 and LNCaP |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MYCBP2 | down-regulates quantity by destabilization
ubiquitination
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-267149 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 32814769 |
We identified several E3 ligases as strong candidates responsible for AR and MYC protein loss as HECTD4, MYCBP2, and TRIM49. HECTD4 and MYCBP2 target AR and MYC for degradation while TRIM49 appears to promote AR and MYC stability. We have shown that these E3 ligases in turn are directly regulated by MYC. MYC in turn represses the expression of ubiquitin ligases, HECTD4 and MYCBP2 that promote AR and MYC protein degradation, further suppressing MYC and AR in a feed forward loop. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
oxandrolone | up-regulates activity
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259265 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10077001 |
The anabolic steroids, oxandrolone and fluoxymesterone, have high inhibition constants for binding, yet induce the N/C interaction and stabilize AR at relatively low ligand concentrations and are AR agonists in vivo. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FKBP4 | up-regulates activity
binding
|
AR |
0.709 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-252034 |
|
|
Mus musculus |
Neuronal Cell Line |
| pmid |
sentence |
| 19545546 |
We noted that FK506 altered nuclear localization of the GR and inhibited expression of GR-responsive genes. Furthermore, si-RNA knockdown of FKBP4 gene, coding for the immunophilin FKBP52, inhibited cortisol-activated GR nuclear translocation |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
UBE2C |
0.408 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251543 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 19632176 |
The evolution of prostate cancer from an androgen-dependent state (ADPCa) to one that is androgen-independent (AIPCa) marks its lethal progression. The androgen receptor (AR) is essential in both, though its function in AIPCa is poorly understood. We have defined the direct AR-dependent target genes in both AIPCa and ADPCa by generating AR-dependent gene expression profiles and AR cistromes. In contrast to ADPCa, AR selectively up-regulates M-phase cell cycle genes in AIPCa including UBE2C, a gene that inactivates the M-phase checkpoint. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
CTNNB1 |
0.719 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-116260 |
|
|
Homo sapiens |
Neuron |
| pmid |
sentence |
| 11916967 |
Transcription assays demonstrated that liganded ar repressed beta-catenin/t cell factor-responsive reporter gene activity |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
17beta-hydroxy-5alpha-androstan-3-one | up-regulates
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251533 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
Testosterone is the predominant circulating androgen in mammals and is converted to dihydrotestosterone (DHT) by 5α-reductase in certain tissues of the male urogenital tract, skin, and other target cells. DHT binds with highest affinity to AR and together with testosterone promotes AR transcriptional activity thereby ensuring the development and maintenance of male reproductive functions. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
perfluorooctanoic acid | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268768 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
NCOA4 | up-regulates
binding
|
AR |
0.854 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-67684 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10347167 |
We demonstrated that ara70 and ar physically interact and that ara70 can function as an androgen-dependent coactivator for ar. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates
|
Differentiation |
0.7 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251538 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
AR homodimers recruit a panoply of factors including coactivators and mediator proteins whose enzymatic activities promote chromatin remodeling and transcriptional regulation of target genes leading to cell differentiation, survival, and proliferation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
4,4'-sulfonyldiphenol | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268733 |
|
|
in vitro |
|
| pmid |
sentence |
| 31995776 |
This study investigated the endocrine-disrupting activity of BPA, BPF, and BPS alone or as a mixture and the agonistic and antagonistic activity of the BPs using an in vitro bioassay to detect ER-, AR-, and AhR-mediated activity. Here, we evaluated the endocrine-disrupting risks of the bisphenols by investigating their agonist and antagonist activities with the estrogen (ER), androgen (AR), and aryl hydrocarbon (AhR) receptors. Our results showed that BPA, BPS, and BPF (BPs) have estrogen agonist and androgen antagonist activities and decrease the ERα protein level. . |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
bisphenol F | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268734 |
|
|
in vitro |
|
| pmid |
sentence |
| 31995776 |
This study investigated the endocrine-disrupting activity of BPA, BPF, and BPS alone or as a mixture and the agonistic and antagonistic activity of the BPs using an in vitro bioassay to detect ER-, AR-, and AhR-mediated activity. Here, we evaluated the endocrine-disrupting risks of the bisphenols by investigating their agonist and antagonist activities with the estrogen (ER), androgen (AR), and aryl hydrocarbon (AhR) receptors. Our results showed that BPA, BPS, and BPF (BPs) have estrogen agonist and androgen antagonist activities and decrease the ERα protein level. . |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
WEE1 |
0.263 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253678 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
TBL1XR1 | up-regulates
binding
|
AR |
0.403 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-203235 |
|
|
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 24243687 |
We showed that tblr1 physically interacts with ar and directly occupies the androgen-response elements of the affected ar target genes in an androgen-dependent manner. / we characterized tblr1 as a coactivator of ar |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
KLK3 |
0.816 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253657 |
|
|
|
|
| pmid |
sentence |
| 20069563 |
TH1 also associates with AR at the active androgen-responsive prostate-specific antigen (PSA) promoter in the nucleus of LNCaP cells. Decrease of endogenous AR protein by TH1 interferes with androgen-induced luciferase reporter expression and reduces endogenous PSA expression. |
|
| Publications: |
1 |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
ARG1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253738 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 20711410 |
The regulation of arginase expression following androgen stimulation was dependent on the androgen receptor (AR), as a siRNA treatment targeting the AR inhibited both ARG1 and ARG2 overexpression. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
NSD2 | up-regulates
binding
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-186045 |
|
|
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 19481544 |
In this study, we discovered that nsd2 specifically interacts with the dna-binding domain of androgen receptor (ar) via its hmg domain, and the nuclear translocation of both nsd2 and ar is enhanced in the presence of ligand / the histone methyltransferase, nsd2, enhances androgen receptor-mediated transcription. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HSP90AA1 | up-regulates activity
binding
|
AR |
0.754 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251536 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
The unliganded AR resides predominately in the cytoplasm as a heteromeric complex with hsp90 and other chaperone proteins. These chaperone proteins maintain AR in a form that is receptive to ligand binding. Regulation of gene expression by androgen-activated AR occurs through receptor nuclear translocation, dimerization, and binding to androgen response elements (AREs) in the DNA of target genes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
tibolone | up-regulates activity
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257823 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 19464167 |
In this study, we have assessed the potential hormonal profile of tibolone and its primary metabolites on all human steroid receptors (PR, AR, GR, MR, ERα and ERβ) using HeLa or PC3 cells stably transfected with a given receptor and a luciferase reporter gene. We show that tibolone and its ∆ 4 -isomer predominantly bind and activate PR and AR whereas 3α and 3β-OH-tibolone predominantly bind and activate ERα (Table 1). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
cyproterone acetate | down-regulates
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191235 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | down-regulates quantity by repression
transcriptional regulation
|
BTG2 |
0.385 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253674 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 16281084 |
After AR antagonist flutamide treatment, three hundred and twenty-six genes (3.93%) expressed differentially, 97 down-regulated and 219 up-regulated. Among them, eight up-regulated genes might be cell cycle-related, namely CDC10, NRAS, BTG1, Wee1, CLK3, DKFZP564A122, CDKN1A and BTG2. The CDKN1A and BTG1 gene mRNA expression was confirmed to be higher in the experimental group by RT-PCR, while p53 mRNA expression had no significant changes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FHL2 | up-regulates
binding
|
AR |
0.538 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-74703 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10654935 |
Fhl2 contains a strong, autonomous transactivation function and binds specifically to the ar in vitro and in vivo. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Prostate Gland |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
ARG2 |
0.266 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253671 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20711410 |
The regulation of arginase expression following androgen stimulation was dependent on the androgen receptor (AR), as a siRNA treatment targeting the AR inhibited both ARG1 and ARG2 overexpression. This observation was correlated in vivo in patients by immunohistochemistry. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates quantity by expression
transcriptional regulation
|
NKX3-1 |
0.518 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251546 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16697957 |
Whereas androgen receptor (AR) positively regulates NKX3.1 expression, NKX3.1 negatively modulates AR transcription and consequently the AR-associated signaling events. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
SRCAP | up-regulates activity
binding
|
AR |
0.42 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-255221 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20432434 |
The SNF2-related CBP activator protein (SRCAP) serves as a coactivator for several nuclear receptors including the androgen receptor (AR). SRCAP is an ATPase that is the core subunit of a large multiprotein complex and was shown to incorporate the histone variant H2A.Z into nucleosomes. In this report, we demonstrate that SRCAP is expressed in the epithelium of normal prostate and in prostate carcinoma cells, and is associated with AR in the nucleus |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
AR | up-regulates
|
Survival |
0.7 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251539 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15861399 |
AR homodimers recruit a panoply of factors including coactivators and mediator proteins whose enzymatic activities promote chromatin remodeling and transcriptional regulation of target genes leading to cell differentiation, survival, and proliferation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Prostate Cancer |
| + |
DAB2IP | down-regulates activity
binding
|
AR |
0.335 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254758 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 27858941 |
DAB2IP acts as a scaffold protein for PP2A to suppress DHT-elicited S81 phosphorylation of the AR, preventing its nuclear translocation and binding to androgen response elements. In addition, DAB2IP can compete with the AR for binding to c-Src, thus blocking the non-genomic AR pathway |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ZNF318 | down-regulates activity
binding
|
AR |
0.379 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261187 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16469430 |
Using different promoters and cells, we confirmed that AR-mediated transactivation was repressed by TZF in a dose-dependent manner (Fig. 1A and B). Endogenous ARmediated transactivation was also inhibited by expression of TZF; These results indicate that amino acid residues 512–663 are essential for the repressive effect of TZF on AR-mediated transactivation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
perfluorohexanesulfonic acid | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268766 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
(2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide | up-regulates
chemical activation
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-189623 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PIM1 | up-regulates activity
phosphorylation
|
AR |
0.391 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277575 |
|
|
Homo sapiens |
LNCaP Cell |
| pmid |
sentence |
| 34697370 |
PIM1 phosphorylates the AR and 14-3-3 ζ and coordinates their interaction. PIM1 phosphorylation of the AR and 14-3-3 ζ enhances their interaction and shifts their occupancy on chromatin, resulting in 14-3-3 ζ co-regulation of AR, likely by recruiting other AR co-regulators such as hnRNPK and TRIM28. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HIP1 | down-regulates quantity by repression
transcriptional regulation
|
AR |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-138820 |
|
|
Homo sapiens |
Prostate Gland Cancer Cell |
| pmid |
sentence |
| 16027218 |
Hip1 as a transcriptional regulator of the ar / silencing hip1 expression reduces the transcriptional activity and protein levels of the ar |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
flutamide | down-regulates activity
chemical inhibition
|
AR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257807 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18571420 |
Among the compounds obtained, N-[4-[(benzyl)(4-nitrophenyl)amino]-1-methylpyrrole-2-carbonyl]pyrrolidine (22) is as potent an AR antagonist as the typical anilide-type AR antagonists hydroxyflutamide and bicalutamide. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
AR
- 
- 