Id: acc1835
Group: 2sens
Protein: p53
Gene Symbol: TP53
Protein Id: P04637
Protein Name: P53_HUMAN
PTM: acetylation
Site: Lys370
Site Sequence: GSRAHSSHLKSKKGQSTSRHK
Disease Category: Cancer
Disease: Colorectal Cancer
Disease Subtype:
Disease Cellline: HCT116
Disease Info:
Drug: MS-275
Drug Info: "MS-275 (Entinostat) is a selective class I histone deacetylase (HDAC) inhibitor that targets HDAC1, HDAC2, and HDAC3, exhibiting potent anti-proliferative activity and inducing apoptosis in various cancer cells, and has entered clinical trials for tumor therapy."
Effect: modulate
Effect Info: "After MS-275 treatment, the interaction between p53 and p21 decreased, the level of highly acetylated C-terminus of p53 increased, and the cooperative regulation of cell invasion and death by p53 and p21 was interfered."
Note: site unclear
Score: 4.0
Pubmed(PMID): 36257192
Sentence Index:
Sentence:

Sequence & Structure:

MEEPQSDPSVEPPLSQETFSDLWKLLPENNVLSPLPSQAMDDLMLSPDDIEQWFTEDPGPDEAPRMPEAAPPVAPAPAAPTPAAPAPAPSWPLSSSVPSQKTYQGSYGFRLGFLHSGTAKSVTCTYSPALNKMFCQLAKTCPVQLWVDSTPPPGTRVRAMAIYKQSQHMTEVVRRCPHHERCSDSDGLAPPQHLIRVEGNLRVEYLDDRNTFRHSVVVPYEPPEVGSDCTTIHYNYMCNSSCMGGMNRRPILTIITLEDSSGNLLGRNSFEVRVCACPGRDRRTEEENLRKKGEPHHELPPGSTKRALPNNTSSSPQPKKKPLDGEYFTLQIRGRERFEMFRELNEALELKDAQAGKEPGGSRAHSSHLKSKKGQSTSRHKKLMFKTEGPDSD

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
TP53 EPRENETAPOPT Cellular tumor antigen p53 stabiliser 3 Completed myelodysplastic syndrome ClinicalTrials
TP53 IDASANUTLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 3 Terminated acute myeloid leukemia ClinicalTrials
TP53 CENERSEN SODIUM p53 mRNA antisense inhibitor 2 Terminated chronic lymphocytic leukemia ClinicalTrials
TP53 CENERSEN p53 mRNA antisense inhibitor 2 Completed acute myeloid leukemia ClinicalTrials
TP53 CENERSEN p53 mRNA antisense inhibitor 2 Withdrawn acute myeloid leukemia ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting essential thrombocythemia ClinicalTrials
TP53 SIREMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting neoplasm ClinicalTrials
TP53 IDASANUTLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting neoplasm ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Terminated small cell lung carcinoma ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Active, not recruiting polycythemia vera ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting polycythemia vera ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting primary myelofibrosis ClinicalTrials
TP53 IDASANUTLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Terminated polycythemia vera ClinicalTrials
TP53 CONTUSUGENE LADENOVEC Cellular tumor antigen p53 exogenous gene 2 Unknown status non-small cell lung carcinoma ClinicalTrials
TP53 APG115 Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting lymphoid leukemia ClinicalTrials
TP53 CONTUSUGENE LADENOVEC Cellular tumor antigen p53 exogenous gene 2 Terminated head and neck malignant neoplasia ClinicalTrials
TP53 CONTUSUGENE LADENOVEC Cellular tumor antigen p53 exogenous gene 2 Unknown status head and neck malignant neoplasia ClinicalTrials
ClinicalTrials
TP53 EPRENETAPOPT Cellular tumor antigen p53 stabiliser 2 Withdrawn Mantle cell lymphoma ClinicalTrials
TP53 TEPRASIRAN p53 mRNA RNAi inhibitor 2 Completed Acute kidney injury ClinicalTrials
TP53 EPRENETAPOPT Cellular tumor antigen p53 stabiliser 2 Completed ovarian cancer ClinicalTrials
TP53 CONTUSUGENE LADENOVEC Cellular tumor antigen p53 exogenous gene 2 Completed breast cancer ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 2 Recruiting endometrial cancer ClinicalTrials
TP53 CENERSEN p53 mRNA antisense inhibitor 1 Terminated myelodysplastic syndrome ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 1 Active, not recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
TP53 NAVTEMADLIN Tumour suppressor p53/oncoprotein Mdm2 inhibitor 1 Completed acute myeloid leukemia 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
TP53-Lys370
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
K 370 D Breast cancer Acetylation 37156774
K 370 U Breast cancer/tumor/carcinoma Methylation 22864287
K 370 U Glioblastoma Methylation 22864287

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: