+ |
ATF4 | up-regulates quantity by expression
transcriptional regulation
|
SIGMAR1 |
0.392 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-253750 |
|
|
Homo sapiens |
|
pmid |
sentence |
22079628 |
we have demonstrated that Sig-1Rs were transcriptionally upregulated by ATF4 in ER stress. |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
3-(4-Methylphenyl)-5-(1-propyl-3,6-dihydro-2H-pyridin-5-yl)-1,2-oxazole | down-regulates activity
chemical inhibition
|
SIGMAR1 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-261114 |
|
|
Mus musculus |
|
pmid |
sentence |
9144641 |
PD144418 exhibited an affinity for ơ1 of 0.08nM(Ki) versusa Ki of 1377nM for ơ2 site. |
|
Publications: |
1 |
Organism: |
Mus Musculus |
+ |
PB28 dihydrochloride | down-regulates activity
chemical inhibition
|
SIGMAR1 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-261111 |
|
|
Homo sapiens |
MCF-7 Cell |
pmid |
sentence |
16891467 |
Cyclohexylpiperazine derivative PB28, a σ2 agonist and σ1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
S1RA | down-regulates activity
chemical inhibition
|
SIGMAR1 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-261122 |
|
|
Homo sapiens |
CACO-2 Cell |
pmid |
sentence |
22784008 |
The most selective compounds were further profiled, and compound 28, 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862) emerged as the most interesting candidate. Compound 28 is a highly selective σ1R antagonist and has successfully completed phase I safety and pharmacokinetic evaluation in humans. |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
(RS)-Ppcc | up-regulates activity
chemical activation
|
SIGMAR1 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-261107 |
|
|
Homo sapiens |
|
pmid |
sentence |
17328523 |
We suggest that 4b may act as a ơ1/ơ2 agonist and that the ơ ligands may modulate TG-2 differently. |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
haloperidol | down-regulates activity
chemical inhibition
|
SIGMAR1 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-261090 |
|
|
Homo sapiens |
SH-SY5Y Cell |
pmid |
sentence |
17419803 |
These results suggest that haloperidol may irreversibly inactivate sigma-1 receptors in guinea pig and human cells, probably after metabolism to reduced haloperidol. |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
SIGMAR1 | up-regulates quantity by stabilization
stabilization
|
CD274 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-274974 |
|
|
Homo sapiens |
MDA-MB-231 Cell |
pmid |
sentence |
29117944 |
We propose that Sigma1 is a ligand-operated scaffolding protein that promotes the stability, processing, assembly, and trafficking of specific proteins in the secretory pathway of cancer cells. In support of this hypothesis, we found that siRNA-mediated knockdown of Sigma1 resulted in a significant decrease in PD-L1 protein levels in triple-negative MDA-MB-231 breast cancer and androgen-independent PC3 prostate cancer cells |
|
Publications: |
1 |
Organism: |
Homo Sapiens |