| Id: | acc3408 |
| Group: | 2sens |
| Protein: | p65 |
| Gene Symbol: | RELA |
| Protein Id: | Q04206 |
| Protein Name: | TF65_HUMAN |
| PTM: | phosphorylation |
| Site: | Ser536 |
| Site Sequence: | LLSGDEDFSSIADMDFSALLS |
| Disease Category: | Immune system diseases |
| Disease: | Rheumatoid Arthritis |
| Disease Subtype: | |
| Disease Cellline: | |
| Disease Info: | |
| Drug: | licochalcone A (LCA) |
| Drug Info: | Licochalcone A (LCA) is a drug that may have certain pharmacological activities. It could potentially be used in medical research and treatment. |
| Effect: | modulate |
| Effect Info: | "Licochalcone A inhibits the phosphorylation and nuclear translocation of the p65 subunit, thereby blocking the NF-κB signaling pathway and exerting an anti-RA effect." |
| Note: | |
| Score: | 4.0 |
| Pubmed(PMID): | 29864947 |
| Sentence Index: | 29864947_5-6 |
| Sentence: | "Interestingly, IKKbeta phosphorylation was not detectable in RASFs, indicating that LCA altered the morphology, ultrastructure and stiffness of the RASF membrane by inhibiting NF-kappaB activation independent of IKKbeta phosphorylation. Antigen-induced arthritis (AIA) was established in Sprague Dawley (SD) rats to validate the anti-arthritic effect of LCA, and LCA significantly decreased both the arthritis scores and paw swelling in the AIA rats, suggesting that LCA inhibits the progression and development of arthritis in vivo." |
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.
