| Id: | acc3419 |
| Group: | 2sens |
| Protein: | p65 |
| Gene Symbol: | RELA |
| Protein Id: | Q04206 |
| Protein Name: | TF65_HUMAN |
| PTM: | phosphorylation |
| Site: | Ser536 |
| Site Sequence: | LLSGDEDFSSIADMDFSALLS |
| Disease Category: | Cancer |
| Disease: | Breast Cancer |
| Disease Subtype: | |
| Disease Cellline: | MCF-7 |
| Disease Info: | |
| Drug: | TRAIL + BIX-01294 |
| Drug Info: | TRAIL is a cytokine that can induce apoptosis in cancer cells | BIX - 01294 is a histone methyltransferase G9a inhibitor. |
| Effect: | modulate |
| Effect Info: | "BIX-01294 alone induces the phosphorylation of p65, but when combined with TRAIL, the phosphorylation level decreases, suggesting the possible existence of different pathway regulations." |
| Note: | "drug comb, Non-conventional drugs" |
| Score: | 3.0 |
| Pubmed(PMID): | 29964331 |
| Sentence Index: | 29964331_2-3 |
| Sentence: | "However, breast cancer cells are generally resistant to TRAIL, thus limiting its therapeutic potential. In this study, we found that BIX-01294, a selective inhibitor of euchromatin histone methyltransferase 2/G9a, is a strong TRAIL sensitizer in breast cancer cells." |
Sequence & Structure:
MDELFPLIFPAEPAQASGPYVEIIEQPKQRGMRFRYKCEGRSAGSIPGERSTDTTKTHPTIKINGYTGPGTVRISLVTKDPPHRPHPHELVGKDCRDGFYEAELCPDRCIHSFQNLGIQCVKKRDLEQAISQRIQTNNNPFQVPIEEQRGDYDLNAVRLCFQVTVRDPSGRPLRLPPVLSHPIFDNRAPNTAELKICRVNRNSGSCLGGDEIFLLCDKVQKEDIEVYFTGPGWEARGSFSQADVHRQVAIVFRTPPYADPSLQAPVRVSMQLRRPSDRELSEPMEFQYLPDTDDRHRIEEKRKRTYETFKSIMKKSPFSGPTDPRPPPRRIAVPSRSSASVPKPAPQPYPFTSSLSTINYDEFPTMVFPSGQISQASALAPAPPQVLPQAPAPAPAPAMVSALAQAPAPVPVLAPGPPQAVAPPAPKPTQAGEGTLSEALLQLQFDDEDLGALLGNSTDPAVFTDLASVDNSEFQQLLNQGIPVAPHTTEPMLMEYPEAITRLVTGAQRPPDPAPAPLGAPGLPNGLLSGDEDFSSIADMDFSALLSQISS
Select PDB:
| Target | Drug name | MOA | Phase | Status | Disease | Source |
|---|---|---|---|---|---|---|
| RELA | EDASALONEXENT | Nuclear factor NF-kappa-B complex inhibitor | 3 | Terminated | Duchenne muscular dystrophy | ClinicalTrials |
| RELA | EDASALONEXENT | Nuclear factor NF-kappa-B complex inhibitor | 3 | Completed | Duchenne muscular dystrophy | ClinicalTrials |
| RELA | EDASALONEXENT | Nuclear factor NF-kappa-B complex inhibitor | 1 | Completed | type 2 diabetes mellitus | ClinicalTrials |
| RELA | EDASALONEXENT | Nuclear factor NF-kappa-B complex inhibitor | 1 | Completed | Duchenne muscular dystrophy | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo intensity data of this site,
show all other sites!
| RELA-Ser112 | |||||
|---|---|---|---|---|---|
| Cancer | Intensity | ||||
| BRCA | |||||
| COAD | |||||
| HGSC | |||||
| ccRCC | 0.367 | ||||
| GBM | |||||
| HNSC | |||||
| LUAD | |||||
| LUSC | 0.765 | ||||
| non_ccRCC | |||||
| PDAC | |||||
| UCEC | -1.132 | ||||
| RELA-Ser177 | |||||
|---|---|---|---|---|---|
| Cancer | Intensity | ||||
| BRCA | |||||
| COAD | |||||
| HGSC | |||||
| ccRCC | 0.675 | ||||
| GBM | -0.474 | ||||
| HNSC | |||||
| LUAD | -0.6 | ||||
| LUSC | -0.083 | ||||
| non_ccRCC | 1.626 | ||||
| PDAC | |||||
| UCEC | -1.143 | ||||
| RELA-Ser200 | |||||
|---|---|---|---|---|---|
| Cancer | Intensity | ||||
| BRCA | |||||
| COAD | 0.131 | ||||
| HGSC | -2.56 | ||||
| ccRCC | 0.526 | ||||
| GBM | 0.516 | ||||
| HNSC | 0.416 | ||||
| LUAD | |||||
| LUSC | 0.737 | ||||
| non_ccRCC | -0.008 | ||||
| PDAC | 0.386 | ||||
| UCEC | -0.143 | ||||
| RELA-Ser202 | |||||
|---|---|---|---|---|---|
| Cancer | Intensity | ||||
| BRCA | |||||
| COAD | |||||
| HGSC | |||||
| ccRCC | |||||
| GBM | 1.142 | ||||
| HNSC | -0.719 | ||||
| LUAD | -0.423 | ||||
| LUSC | |||||
| non_ccRCC | |||||
| PDAC | |||||
| UCEC | |||||
| RELA-Ser235 | |||||
|---|---|---|---|---|---|
| Cancer | Intensity | ||||
| BRCA | -0.452 | ||||
| COAD | -0.397 | ||||
| HGSC | 2.387 | ||||
| ccRCC | -0.206 | ||||
| GBM | -0.643 | ||||
| HNSC | 0.08 | ||||
| LUAD | -0.689 | ||||
| LUSC | 0.666 | ||||
| non_ccRCC | |||||
| PDAC | |||||
| UCEC | -0.747 | ||||
| RELA-Ser42 | |||||
|---|---|---|---|---|---|
| Cancer | Intensity | ||||
| BRCA | |||||
| COAD | |||||
| HGSC | |||||
| ccRCC | 0.381 | ||||
| GBM | -1.76 | ||||
| HNSC | 0.615 | ||||
| LUAD | 0.173 | ||||
| LUSC | |||||
| non_ccRCC | |||||
| PDAC | |||||
| UCEC | 0.591 | ||||
| RELA-Ser45 | |
|---|---|
| Cancer | Intensity |
| BRCA | |
| COAD | |
| HGSC | -0.868 |
| ccRCC | -0.94 |
| GBM | |
| HNSC | 1.524 |
| LUAD | |
| LUSC | |
| non_ccRCC | |
| PDAC | 0.148 |
| UCEC | 0.137 |
PTM-Disease Association:
source: PTMD| Residue | Position | State | Disease | Class | PMID |
|---|---|---|---|---|---|
| S | 536 | P | Hepatocellular carcinoma | Phosphorylation | 34380537 |
| S | 536 | P | Glioblastoma | Phosphorylation | 36116131 |
| S | 536 | U | Pancreatic ductal adenocarcinoma | Phosphorylation | 29363544 |
| S | 536 | U | Colonic inflammation | Phosphorylation | 34803708 |
| S | 536 | U | Hepatocellular carcinoma/hepatocarcinoma/hepatoma | Phosphorylation | 20224721 |
| S | 536 | U | Oral squamous cell carcinoma | Phosphorylation | 24063540 |
State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.
