PMADS

Id:	acc3724
Group:	1sens
Protein:	H2AX
Gene Symbol:	H2AX
Protein Id:	P16104
Protein Name:	H2AX_HUMAN
PTM:	phosphorylation
Site:	unclear
Site Sequence:
Disease Category:	Cancer
Disease:	Ovarian Cancer
Disease Subtype:	Tumor Apoptosis
Disease Cellline:	IGROV-1
Disease Info:
Drug:	ST1926+ZD1839
Drug Info:	ST1926 is one of the drugs in the combination \| ZD1839 is the other drug combined with ST1926.
Effect:	modulate
Effect Info:	Combined therapy enhances γ-H2AX phosphorylation and promotes tumor cell death.
Note:	histone
Score:	3.0
Pubmed(PMID):	15781651
Sentence Index:	15781651_5
Sentence:	"Other molecular events induced by the cotreatment included (a) a stabilization of the ST1926-induced genotoxic stress detected by formation of phosphorylated gamma-H2AX foci and (b) a complete inhibition of extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation associated with activation of the proapoptotic protein BAD (i.e., inhibition of phosphorylation on Ser112)."

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
S	139	U	Acute myelogenous leukemia	Phosphorylation	33691101
S	139	U	Hepatocellular carcinoma	Phosphorylation	25537504
S	139	U	Multiple myeloma	Phosphorylation	35190641

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:

CTD
DMRdb