Id: acc2473
Group: 2sens
Protein: p53
Gene Symbol: TP53
Protein Id: P04637
Protein Name: P53_HUMAN
PTM: phosphorylation
Site: Ser392
Site Sequence: LMFKTEGPDSD----------
Disease Category: Cancer
Disease: Melanoma
Disease Subtype:
Disease Cellline: SK-Mel-28
Disease Info:
Drug: dacarbazine
Drug Info: "Dacarbazine is an alkylating antineoplastic agent primarily used for treating malignant melanoma, Hodgkin's lymphoma, and soft tissue sarcomas, functioning by alkylating DNA and inhibiting purine and RNA synthesis to exert cytotoxic effects on tumor cells."
Effect: promote
Effect Info: Qct enhanced the sensitivity of melanoma cells to DTIC by activating the phosphorylation of ATM and p53.
Note:
Score: 5.0
Pubmed(PMID): 18791269
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TP53 CENERSEN p53 mRNA antisense inhibitor 2 Withdrawn acute myeloid leukemia ClinicalTrials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-Ser392
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
S 392 A Breast cancer/tumor/carcinoma Phosphorylation 21084272
S 392 P Vestibular schwannomas Phosphorylation 16299809
S 392 U Hepatocellular carcinoma/hepatocarcinoma/hepatoma Phosphorylation 21455220
S 392 U Ovarian cancer/carcinoma Phosphorylation 20009884
S 392 U Lung adenocarcinoma Phosphorylation 32181328

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P04637 TP53 P Ser392 LMFKTEGPDS(ph)D RPMI8226 BTZ 10.2047 -
P04637 TP53 P Ser392 LMFKTEGPDS(ph)D RPMI8226 BTZ 9.4965 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: