Id: | acc2155 |
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: | Ovarian Cancer |
Disease Subtype: | |
Disease Cellline: | HEY/C-2 |
Disease Info: | |
Drug: | Cisplatin |
Drug Info: | "Cisplatin is a platinum-based chemotherapeutic agent widely used in the treatment of various malignancies, including ovarian, bladder, testicular, and non-small cell lung cancers, by forming DNA cross-links to interfere with replication and repair, thereby inhibiting cancer cell growth and proliferation." |
Effect: | increase |
Effect Info: | "In cisplatin-resistant cells, the ability of CDDP to induce the expression and phosphorylation of p53 is reduced." |
Note: | |
Score: | 5.0 |
Pubmed(PMID): | 14513366 |
Sentence Index: | 14513366_2-3 |
Sentence: | "In this article we examine DNA damage-induced phosphorylation of p53 and downstream p53-dependent transactivation events in cisplatin-sensitive and cisplatin-resistant human cancer cell lines possessing wild-type p53. METHODS: Western-blot analysis was utilized to study the effect of cisplatin and the analog on p53 phosphorylation and p53-dependent target genes. RESULTS: In response to CDDP and DACH-Ac-Pt, both CDDP-sensitive and CDDP-resistant models demonstrated time- and dose-dependent inductions of total p53 protein and an increase in Ser-15 phosphorylation, which was more pronounced with CDDP." |
Sequence & Structure:
MEEPQSDPSVEPPLSQETFSDLWKLLPENNVLSPLPSQAMDDLMLSPDDIEQWFTEDPGPDEAPRMPEAAPPVAPAPAAPTPAAPAPAPSWPLSSSVPSQKTYQGSYGFRLGFLHSGTAKSVTCTYSPALNKMFCQLAKTCPVQLWVDSTPPPGTRVRAMAIYKQSQHMTEVVRRCPHHERCSDSDGLAPPQHLIRVEGNLRVEYLDDRNTFRHSVVVPYEPPEVGSDCTTIHYNYMCNSSCMGGMNRRPILTIITLEDSSGNLLGRNSFEVRVCACPGRDRRTEEENLRKKGEPHHELPPGSTKRALPNNTSSSPQPKKKPLDGEYFTLQIRGRERFEMFRELNEALELKDAQAGKEPGGSRAHSSHLKSKKGQSTSRHKKLMFKTEGPDSD
Select PDB:
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 TargetsPTM Intensity:
source: CPTACTP53-Ser392 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDResidue | 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: DecryptMProtein | 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: funscoRNo data.