Id: | acc1804 |
Group: | 2sens |
Protein: | p65 |
Gene Symbol: | RELA |
Protein Id: | Q04206 |
Protein Name: | TF65_HUMAN |
PTM: | acetylation |
Site: | Lys310 |
Site Sequence: | KRKRTYETFKSIMKKSPFSGP |
Disease Category: | Cancer |
Disease: | Pancreas Cancer |
Disease Subtype: | PDAC |
Disease Cellline: | PANC-1 |
Disease Info: | |
Drug: | ICB |
Drug Info: | - |
Effect: | sensitize |
Effect Info: | HDAC5 also reduces the acetylation of p65 at lysine-310. Silencing or inhibiting HDAC5 can render PDAC tumors sensitive to immune checkpoint blockade (ICB) therapy. |
Note: | Non-conventional drugs |
Score: | 4.5 |
Pubmed(PMID): | 35265200 |
Sentence Index: | 35265200_11-12 |
Sentence: | "Additionally, HDAC5 diminished p65 acetylation at lysine-310, which is essential for the transcriptional activity of p65. Importantly, we demonstrated that HDAC5 silencing or inhibition sensitized PDAC tumors to immune checkpoint blockade (ICB) therapy in syngeneic mouse model and KPC mouse derived PDAC model." |
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-Lys122 | |||||
---|---|---|---|---|---|
Cancer | Intensity | ||||
BRCA | -0.78 | ||||
COAD | |||||
HGSC | |||||
ccRCC | |||||
GBM | -1.123 | ||||
HNSC | |||||
LUAD | 0.137 | ||||
LUSC | 0.357 | ||||
non_ccRCC | |||||
PDAC | |||||
UCEC | 1.409 |
RELA-Lys123 | |||||
---|---|---|---|---|---|
Cancer | Intensity | ||||
BRCA | 0.707 | ||||
COAD | |||||
HGSC | |||||
ccRCC | |||||
GBM | |||||
HNSC | |||||
LUAD | |||||
LUSC | -0.707 | ||||
non_ccRCC | |||||
PDAC | |||||
UCEC |
RELA-Lys215 | |||||
---|---|---|---|---|---|
Cancer | Intensity | ||||
BRCA | 0.707 | ||||
COAD | |||||
HGSC | |||||
ccRCC | |||||
GBM | |||||
HNSC | |||||
LUAD | |||||
LUSC | |||||
non_ccRCC | |||||
PDAC | |||||
UCEC | -0.707 |
RELA-Lys307 | |
---|---|
Cancer | Intensity |
BRCA | -0.987 |
COAD | |
HGSC | |
ccRCC | |
GBM | |
HNSC | |
LUAD | -0.026 |
LUSC | 1.013 |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
K | 310 | D | Colitis | Acetylation | 35200626 |
K | 310 | D | Non-small cell lung cancer | Acetylation | 29535539 |
K | 310 | D | Pancreatic ductal adenocarcinoma | Acetylation | 35265200 |
K | 310 | U | Esophageal squamous cell carcinoma | Acetylation | 32282366 |
K | 310 | U | Lung cancer | Acetylation | 19345327 |
K | 310 | U | Triple-negative breast cancer | Methylation | 29487338 |
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.