| + |
PKC | up-regulates activity 
dephosphorylation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272512 |
Ser661 |
SSNDSRSsLIRKRST |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272513 |
Ser667 |
SSLIRKRsTRRSVRG |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272514 |
Ser671 |
RKRSTRRsVRGSQAQ |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
PPP5C | down-regulates activity 
dephosphorylation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272505 |
Ser661 |
SSNDSRSsLIRKRST |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272506 |
Ser667 |
SSLIRKRsTRRSVRG |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272507 |
Ser671 |
RKRSTRRsVRGSQAQ |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
PKA | up-regulates activity
dephosphorylation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272508 |
Ser667 |
SSLIRKRsTRRSVRG |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272509 |
Ser671 |
RKRSTRRsVRGSQAQ |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272510 |
Ser683 |
QAQDRKLsTKEALDE |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
PIM1 | up-regulates activity
dephosphorylation
|
ABCB1 |
0.449 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272511 |
Ser683 |
QAQDRKLsTKEALDE |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 24333728 |
Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function|P-gp is known to be phosphorylated at Ser667, Ser671, and Ser683 by PKA; at Ser661, Ser667, and Ser671 by PKC; and at Ser683 by Pim-1|simultaneous expression of PP5 and PPP2R3C reduced the phosphorylation detected by the antibodies that specifically recognize serine/threonine phosphorylated by PKA or serine phosphorylated by PKC. These results suggest that the PP5/PPP2R3C complex dephosphorylates PKA- and PKC-phosphorylated serine residues on P-gp |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
SP1 | up-regulates quantity by expression 
transcriptional regulation
|
ABCB1 |
0.268 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253872 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10644769 |
these results indicate a role for both NF-Y and Sp1 in the transcriptional activation of the MDR1 gene by genotoxic stress, and indicate that YB-1, if involved, is not sufficient to mediate this activation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
SIRT1 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.26 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-255139 |
|
|
Homo sapiens |
MCF-7 Cell |
| pmid |
sentence |
| 20713551 |
Overexpression of SIRT1 enhanced both FoxO reporter activity and nuclear levels of FoxO1. Protein expression of MDR1 and gene transcriptional activity were also up-regulated by SIRT1 overexpression. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
CEBPB | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.454 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253771 |
|
|
Homo sapiens |
MCF-7 Cell |
| pmid |
sentence |
| 15044620 |
C/EBPbeta activates the endogenous MDR1 gene of MCF-7 cells, and this activation was associated with a novel C/EBPbeta interaction region within the proximal MDR1 promoter (-128 to -75). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FBXO21 | down-regulates quantity by destabilization
binding
|
ABCB1 |
0.33 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272422 |
|
|
in vitro |
|
| pmid |
sentence |
| 26299618 |
Here we demonstrate that a ubiquitin E3-ligase, FBXO21, targets the multidrug resistance transporter, ABCB1, also known as P-glycoprotein (P-gp), for proteasomal degradation.Purified in vitro translated FLAG-tagged P-gp along with E2 (UbcH5c), E3 ligase FBXO21, Cul1, Skp1, Roc1 purified from Sf-9 insect cells were incubated in vitro. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
EGR1 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.373 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253871 |
|
|
Homo sapiens |
Hematopoietic Cell |
| pmid |
sentence |
| 7565762 |
TPA induced EGR1 binding to the -69/+20 promoter sequences over a time course which correlated with increased MDR1 promoter activity and increased steady-state MDR1 RNA levels. These data suggest a role for EGR1 in modulating MDR1 promoter activity in hematopoietic cells. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HIF1A | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.306 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254420 |
|
|
Homo sapiens |
Microvascular Endothelial Cell |
| pmid |
sentence |
| 12067980 |
Examination of the MDR1 gene identified a binding site for hypoxia inducible factor-1 (HIF-1), and inhibition of HIF-1 expression by antisense oligonucleotides resulted in significant inhibition of hypoxia-inducible MDR1 expression and a nearly complete loss of basal MDR1 expression. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MECP2 | down-regulates quantity by repression 
transcriptional regulation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254033 |
|
|
|
|
| pmid |
sentence |
| 11865062 |
We have established that methyl-CpG binding protein 2 (MeCP2) is involved in methylation-dependent silencing of human MDR1 in cells that lack the known transcriptional repressors MBD2 and MBD3. In the repressed state the MDR1 promoter is methylated and assembled into chromatin enriched with MeCP2 and deacetylated histone. TSA induced significant acetylation of histones H3 and H4 but did not activate transcription. 5aC induced DNA demethylation, leading to the release of MeCP2, promoter acetylation, and partial relief of repression |
|
| Publications: |
1 |
| + |
HDAC1 | down-regulates quantity by repression
transcriptional regulation
|
ABCB1 |
0.291 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254223 |
|
|
Homo sapiens |
MCF-7/adr Cell |
| pmid |
sentence |
| 20037778 |
we find UHRF1 plays an important role in inhibiting MDR1 promoter activity by directly binding to the MDR1 promoter. Overexpression of UHRF1 in NCI/ADR-RES cells can induce deacetylation of histones H3 and H4 on the MDR1 promoter, which is facilitated by recruitment of HDAC1 to the MDR1 promoter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
JUN | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.35 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254534 |
|
|
Homo sapiens |
MCF-7 Cell |
| pmid |
sentence |
| 10369069 |
Co-transfection of WT cells with a c-jun expression vector and either of the AP-1 luciferase constructs demonstrated that c-jun could activate gene expression from both the consensus and the MDR1 AP-1 sites in a dose dependent manner. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Cullin 1-RBX1-Skp1 | down-regulates quantity by destabilization
polyubiquitination
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-272425 |
|
|
in vitro |
|
| pmid |
sentence |
| 26299618 |
Here we demonstrate that a ubiquitin E3-ligase, FBXO21, targets the multidrug resistance transporter, ABCB1, also known as P-glycoprotein (P-gp), for proteasomal degradation.Purified in vitro translated FLAG-tagged P-gp along with E2 (UbcH5c), E3 ligase FBXO21, Cul1, Skp1, Roc1 purified from Sf-9 insect cells were incubated in vitro. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
TP53 | down-regulates quantity by repression
transcriptional regulation
|
ABCB1 |
0.6 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-255435 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10029407 |
p53 transcriptionally activates expression of the genes encoding epidermal growth factor receptor, matrix metalloproteinase (MMP)-2, cathepsin D, and thrombospondin-1 but represses expression of the genes encoding basic fibroblast growth factor and multidrug resistance-1. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
YBX1 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.39 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253873 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10644769 |
these results indicate a role for both NF-Y and Sp1 in the transcriptional activation of the MDR1 gene by genotoxic stress, and indicate that YB-1, if involved, is not sufficient to mediate this activation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MYCN | down-regulates quantity by repression
transcriptional regulation
|
ABCB1 |
0.376 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254616 |
|
|
Homo sapiens |
SH-SY5Y Cell, BE(2)-M17 Cell |
| pmid |
sentence |
| 7923112 |
Decreased expression of the N-myc oncogene in neuroblastoma cell lines SH-SY5Y and BE(2)-C, following treatment with retinoic acid, was paralleled by down-regulation of MRP gene expression, contrasting with increased expression of the MDR1 gene. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
EAPP | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253842 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23542036 |
We show here that EAPP stimulates the MDR1 promoter resulting in higher PGP levels. Independently of EAPP, E2F1 also increases the activity of the MDR1 promoter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
TCF4 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.251 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-255389 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20459685 |
Cd2+ reduced the interaction of beta-catenin with AJ components (E-cadherin, alpha-catenin) and increased binding to the transcription factor TCF4 of the Wnt pathway, which was upregulated and translocated to the nucleus. While Wnt target genes (c-Myc, cyclin D1 and ABCB1) were up-regulated by Cd2+, electromobility shift assays showed increased TCF4 binding to cyclin D1 and ABCB1 promoter sequences with Cd2+. Overexpression of wild-type and mutant TCF4 confirmed Cd2+-induced Wnt signaling. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
E2F1 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253841 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23542036 |
We show here that EAPP stimulates the MDR1 promoter resulting in higher PGP levels. Independently of EAPP, E2F1 also increases the activity of the MDR1 promoter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
UHRF1 | down-regulates quantity by repression
transcriptional regulation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254224 |
|
|
Homo sapiens |
MCF-7/adr Cell |
| pmid |
sentence |
| 20037778 |
we find UHRF1 plays an important role in inhibiting MDR1 promoter activity by directly binding to the MDR1 promoter. Overexpression of UHRF1 in NCI/ADR-RES cells can induce deacetylation of histones H3 and H4 on the MDR1 promoter, which is facilitated by recruitment of HDAC1 to the MDR1 promoter. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
DCTPP1 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.334 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261178 |
|
|
Homo sapiens |
BGC-823 Cell |
| pmid |
sentence |
| 27612427 |
DCTPP1 attenuates the sensitivity of human gastric cancer cells to 5-fluorouracil by up-regulating MDR1 expression epigenetically; Moreover, low expression of DCTPP1 led to the increase in intracellular 5-methyl-dCTP, which was strongly associated with the promoter hyper-methylation, leading to the subsequent low-expression of MDR1 and the increased intracellular accumulation of 5-FU in DCTPP1-knockdown BGC-823 cells. These results provide new insights into the roles of DCTPP1 as a chemosensitizer in clinical application. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ETS1 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254077 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20392592 |
High ETS1 expression levels in all resistant MCF-7 sublines may lead to the upregulation of the transcription of MDR1 gene. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FZD7 | up-regulates quantity by expression
post transcriptional regulation
|
ABCB1 |
0.275 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277983 |
|
|
Homo sapiens |
BEL-7402 Cell |
| pmid |
sentence |
| 24018051 |
Knockdown of FZD7 led to decrease the expressions of the MDR1 mRNA and P-gp protein, indicating that FZD7 is involved in the regulation of multidrug resistance in HCC. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
hsa-miR-124-5p | down-regulates quantity by repression
post transcriptional regulation
|
ABCB1 |
0.4 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277970 |
|
|
Homo sapiens |
Caki-2 Cell |
| pmid |
sentence |
| 25861751 |
The current study showed that miR-124 was downregulated in vinblastine- and doxorubicin-resistant renal cancer cells, accompanied by increased levels of FZD5 and P-gp. | Meanwhile, miR-124 targeted FZD5 and abolished its presentation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
YBX1 | down-regulates quantity by repression
transcriptional regulation
|
ABCB1 |
0.39 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-255614 |
|
|
Homo sapiens |
Ovary Cancer Cell |
| pmid |
sentence |
| 17072343 |
YB-1 knockdown by siRNA upregulated 344 genes, including MDR1, thymidylate synthetase, S100 calcium binding protein and cyclin B, and downregulated 534 genes, including CXCR4, N-myc downstream regulated gene 1, E-cadherin and phospholipase C. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
POLR1H | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259907 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 16373708 |
ZNRD1 could significantly up-regulate the expression of P-gp, Bcl-2, and the transcription of the MDR1 gene but not alter the expression of MDR-associated protein, glutathione S-transferase activity, or intracellular glutathione content in leukemia cells. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
NfKb-p65/p50 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.264 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254654 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 19763573 |
PSC833, cyclosporine analogue, downregulates MDR1 expression by activating JNK/c-Jun/AP-1 and suppressing NF-kappaB. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
NR1I2 | up-regulates quantity by expression
transcriptional regulation
|
ABCB1 |
0.468 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-254834 |
|
|
Homo sapiens |
Intestinal Cell Line |
| pmid |
sentence |
| 18540626 |
Among approximately 40 kinds of phytochemicals, tangeretin and ginkgolides A and B markedly induced the PXR-dependent transcriptional activity and also the activity of the human MDR1 promoter. The expression levels of MDR1 mRNA as well as of CYP3A4 mRNA, another gene regulated by PXR, were significantly increased by these phytochemicals. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
regorafenib | down-regulates activity
chemical inhibition
|
ABCB1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259182 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 26254357 |
It is suggested that in vitro, regorafenib is an inhibitor of ABCB1 and ABCG2, but not a substrate, and that its active metabolites, M2 (N-Oxide metabolite) and M5 (N-Oxide/N-desmethyl metabolite), are substrates of ABCB1 and ABCG2 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
ABCB1
- 
- 