PMADS

Id:	acc3373
Group:	2sens
Protein:	H2AX
Gene Symbol:	H2AX
Protein Id:	P16104
Protein Name:	H2AX_HUMAN
PTM:	phosphorylation
Site:	Ser139
Site Sequence:	PSGGKKATQASQEY-------
Disease Category:	Cancer
Disease:	Prostate Cancer
Disease Subtype:
Disease Cellline:	DU145
Disease Info:
Drug:	Etoposide
Drug Info:	"Etoposide is a chemotherapy drug used to treat various types of cancer, such as lung cancer and testicular cancer."
Effect:	modulate
Effect Info:	"The bystander effect induced by DNA damage is transmitted via MVs, leading to an increase in the phosphorylation of H2AX at Ser139 in recipient cells, which indicates an increase in DNA double - strand breaks."
Note:	histone
Score:	3.0
Pubmed(PMID):	28387728
Sentence Index:	28387728_3-4
Sentence:	We report here that etoposide and ultraviolet (UV) exposure stimulate the production of microvesicles (MVs) in DU145 prostate cancer cells. MVs isolated from UV-treated DU145 and A431 epidermoid carcinoma cells as well as etoposide-treated DU145 cells induced phosphorylation of ataxia-telangiectasia mutated (ATM) at serine 1981 (indicative of ATM activation) and phosphorylation of histone H2AX at serine 139 (gammaH2AX) in naive DU145 cells.

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
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