Id: acc1833
Group: 2sens
Protein: NF-kappaB's RelA
Gene Symbol: RELA
Protein Id: Q04206
Protein Name: TF65_HUMAN
PTM: acetylation
Site: Lys310
Site Sequence: KRKRTYETFKSIMKKSPFSGP
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype: TNBC
Disease Cellline: MDA-MB-231
Disease Info:
Drug: 13a
Drug Info: "13a is an optimized BRD4 inhibitor, specifically a 7-methoxy-biscoumarin derivative, designed to selectively target the BD2 domain of BRD4, effectively suppressing NF-κB-driven triple-negative breast cancer cells."
Effect: modulate
Effect Info: "Compound 13a inhibits NF-κB signaling by blocking the interaction between BRD4 and acetylated RelA, thereby impeding the transcription of downstream genes."
Note:
Score: 4.0
Pubmed(PMID): 34378541
Sentence Index:
Sentence:

Sequence & Structure:

MDELFPLIFPAEPAQASGPYVEIIEQPKQRGMRFRYKCEGRSAGSIPGERSTDTTKTHPTIKINGYTGPGTVRISLVTKDPPHRPHPHELVGKDCRDGFYEAELCPDRCIHSFQNLGIQCVKKRDLEQAISQRIQTNNNPFQVPIEEQRGDYDLNAVRLCFQVTVRDPSGRPLRLPPVLSHPIFDNRAPNTAELKICRVNRNSGSCLGGDEIFLLCDKVQKEDIEVYFTGPGWEARGSFSQADVHRQVAIVFRTPPYADPSLQAPVRVSMQLRRPSDRELSEPMEFQYLPDTDDRHRIEEKRKRTYETFKSIMKKSPFSGPTDPRPPPRRIAVPSRSSASVPKPAPQPYPFTSSLSTINYDEFPTMVFPSGQISQASALAPAPPQVLPQAPAPAPAPAMVSALAQAPAPVPVLAPGPPQAVAPPAPKPTQAGEGTLSEALLQLQFDDEDLGALLGNSTDPAVFTDLASVDNSEFQQLLNQGIPVAPHTTEPMLMEYPEAITRLVTGAQRPPDPAPAPLGAPGLPNGLLSGDEDFSSIADMDFSALLSQISS

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

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 Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No 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: PTMD
Residue 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: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: