Id: acc2401
Group: 2sens
Protein: H2AX
Gene Symbol: H2AX
Protein Id: P16104
Protein Name: H2AX_HUMAN
PTM: methylation
Site: Lys134
Site Sequence: VGPKAPSGGKKATQASQEY--
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: A549
Disease Info:
Drug: OTS193320
Drug Info: "OTS193320 is a potent inhibitor of the protein methyltransferase SUV39H2 with an IC50 of 22.2 nM, significantly reducing global H3K9 trimethylation (H3K9me3) and inducing apoptotic cell death in breast cancer cells, while also inhibiting growth in SUV39H2-positive A549 lung cancer cells with an IC50 of 0.38 μM."
Effect: modulate
Effect Info: "The protein methyltransferase SUV39H2 can methylate lysine 134 of histone H2AX and enhance the formation of phosphorylated H2AX (gamma-H2AX), leading to chemoresistance in cancer cells."
Note: histone
Score: 3.0
Pubmed(PMID): 30159125
Sentence Index:
Sentence:

Sequence & Structure:

MSGRGKTGGKARAKAKSRSSRAGLQFPVGRVHRLLRKGHYAERVGAGAPVYLAAVLEYLTAEILELAGNAARDNKKTRIIPRHLQLAIRNDEELNKLLGGVTIAQGGVLPNIQAVLLPKKTSATVGPKAPSGGKKATQASQEY

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

No data.

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 data.

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
K 134 U Bladder cancer Methylation 25487737
K 134 U Lung cancer Methylation 25487737

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: