Id: acc2135
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: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: HCC-827
Disease Info:
Drug: MX-C4
Drug Info: -
Effect: modulate
Effect Info: The small molecule MX-C4 can effectively activate the phosphorylation of p53 in non-small cell lung cancer and exhibits remarkable anti-tumor activity.
Note:
Score: 4.0
Pubmed(PMID): 35902040
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TP53 CENERSEN p53 mRNA antisense inhibitor 2 Withdrawn acute myeloid leukemia ClinicalTrials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: