Id: acc0594
Group: 1sens
Protein: P53
Gene Symbol: TP53
Protein Id: P04637
Protein Name: P53_HUMAN
PTM: phosphorylation
Site: Ser315
Site Sequence: RALPNNTSSSPQPKKKPLDGE
Disease Category: Cancer
Disease: Pancreas Cancer
Disease Subtype:
Disease Cellline: SW1990
Disease Info:
Drug: sodium cantharidinate
Drug Info: "Sodium cantharidinate is a semi-synthetic derivative of cantharidin, primarily used as an antitumor agent in the treatment of hepatocellular carcinoma, with reduced toxicity compared to its parent compound."
Effect: modulate
Effect Info: "Sodium ftibamzone can reduce the phosphorylation level of MDM2 and simultaneously increase the level of phosphorylated p53, thereby inducing apoptosis of pancreatic cancer cells."
Note:
Score: 4.0
Pubmed(PMID): 33165811
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TP53 CENERSEN p53 mRNA antisense inhibitor 2 Withdrawn acute myeloid leukemia ClinicalTrials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-Ser315
Cancer Intensity
BRCA
COAD -1.105
HGSC 0.842
ccRCC 0.263
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 23 A B-cell tumor Phosphorylation 15343266
- - A Colorectal cancer Ubiquitination 37438558
- - A Cervical cancer Ubiquitination 30674441
S 312 A Lymphoma Phosphorylation 24173284
S 392 A Breast cancer/tumor/carcinoma Phosphorylation 21084272
- - A Pancreatic ductal adenocarcinoma Phosphorylation 36209169
K 382 A Osteosarcoma Acetylation 30454890
S 20 A Breast cancer/tumor/carcinoma Phosphorylation 23798621
S 15 A Breast cancer/tumor/carcinoma Phosphorylation 23798621
R 249 C Hepatocellular carcinoma Phosphorylation 29225033 ;  31747859
K 372 D Lymphoma Methylation 24189068
- - D Acute myeloid leukemia Acetylation 29501566
S 15 D Ataxia-telangiectasia Phosphorylation 9733515
S 46 D Psoriasis Phosphorylation 34201431
S 46 D Acute lymphoblastic leukemia Phosphorylation 16377624 ;  23717325
S 15 D Brain cancer Phosphorylation 23268709
S 15 D Breast cancer/tumor/carcinoma Phosphorylation 15958581
S 46 D Breast cancer/tumor/carcinoma Phosphorylation 17404016
S 46 D Hepatocellular cancer Phosphorylation 35227287
S 46 D Colorectal cancer Phosphorylation 37776195
- - D Non-small cell lung cancer Ubiquitination 32248621
- - D Breast cancer Ubiquitination 32571254
- - D Ovarian cancer Ubiquitination 31570706
- - D Ovarian cancer Ubiquitination 32869837
- - D Acute kidney injury Ubiquitination 32248569
K 382 D Neuroblastoma Acetylation 29609003
K 351 D Lung adenocarcinoma Acetylation 37018198
K 373 D Breast cancer Acetylation 37156774
K 372 D Breast cancer Acetylation 37156774
K 373 D Hepatocellular carcinoma Acetylation 37963859
K 382 D Cutaneous melanoma Acetylation 29235570
K 370 D Breast cancer Acetylation 37156774
- - D Breast cancer/tumor/carcinoma Acetylation 24920214
K 305 D Cervical adenocarcinoma Acetylation 32976537
- - D Cardiac fibrosis Acetylation 37408261
K 382 D Acute kidney injury Acetylation 37354967
K 120 D Hepatocellular cancer Acetylation 29174981
K 382 D Cervical adenocarcinoma Acetylation 32976537
K 382 D Osteoporosis Acetylation 37023393
K 387 D Colorectal cancer Acetylation 34847407
S 37 N T-cell lymphoma Phosphorylation 11042698
S 392 P Vestibular schwannomas Phosphorylation 16299809
S 15 P Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 23359208
- - P Lung cancer Ubiquitination 33328571
- - P Renal cell carcinoma Ubiquitination 30874541
- - P Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 23845906
- - P Head and neck squamous cell carcinoma Phosphorylation 23414419
- - P Cervical cancer Ubiquitination 32203172
- - P Breast cancer Ubiquitination 34240781
- - P Melanoma Phosphorylation 22968364
- - P Hepatocellular carcinoma Ubiquitination 34775479
- - P Esophageal squamous cell carcinoma Ubiquitination 32066565
- - P Hepatocellular carcinoma Ubiquitination 31626714
- - P Nasopharyngeal carcinoma Ubiquitination 35517429
- - P Hepatocellular carcinoma/hepatocarcinoma/hepatoma Ubiquitination 16581249
R 213 P Lung cancer/carcinoma Methylation 24384472
- - P Gastric cancer Ubiquitination 24240108
- - U Renal cell carcinoma Ubiquitination 33622324
- - U Hepatocellular carcinoma Ubiquitination 29928880
- - U Lung cancer Ubiquitination 31138778
- - U Colorectal cancer Ubiquitination 33149608
K 382 U Triple-negative breast cancer Acetylation 29334665
- - U Hepatocellular carcinoma Ubiquitination 37460074
- - U Cervical cancer Ubiquitination 35402260
- - U Cancer Ubiquitination 35150809
- - U Hepatocellular carcinoma Ubiquitination 36252649
K 320 U Non-small cell lung cancer Acetylation 29103158
K 381 U Epithelial ovarian cancer Ubiquitination 31002112
K 382 U Epithelial ovarian cancer Ubiquitination 31002112
K 386 U Epithelial ovarian cancer Ubiquitination 31002112
- - U Liver fibrosis Ubiquitination 37495427
- - U Cutaneous T-cell lymphoma Acetylation 32119867
S 392 U Ovarian cancer/carcinoma Phosphorylation 20009884
K 370 U Glioblastoma Methylation 22864287
K 382 U Lung cancer Acetylation 34947995
K 373 U Lung cancer Neddylation 37668436
- - U Breast cancer Neddylation 25867061
S 15 U Down syndrome Phosphorylation 20696760
S 15 U Hepatocellular carcinoma Phosphorylation 22030623
S 15 U Neuroblastoma Phosphorylation 23824039
S 20 U Neuroblastoma Phosphorylation 23824039
S 20 U Ovarian cancer/carcinoma Phosphorylation 20009884
S 46 U Huntington's disease Phosphorylation 22011578
S 392 U Hepatocellular carcinoma/hepatocarcinoma/hepatoma Phosphorylation 21455220
- - U Lung adenocarcinoma Ubiquitination 32553631
S 392 U Lung adenocarcinoma Phosphorylation 32181328
- - U Colon cancer Phosphorylation 35328513
S 15 U Colorectal cancer Phosphorylation 25860929
K 120 U Ovarian cancer Acetylation 28737768
K 370 U Breast cancer/tumor/carcinoma Methylation 22864287
K 382 U Non-small cell lung cancer Acetylation 29103158
K 382 U Hepatocellular carcinoma Acetylation 31440094
K 373 U Triple-negative breast cancer Acetylation 29334665
- - U Colorectal cancer Ubiquitination 31521611
- - U Lung cancer Ubiquitination 31279706
- - U Colorectal cancer Ubiquitination 31239268

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 Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 9.2663 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.2924 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -0.4468 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -3.2215 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.4438 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.8181 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.5314 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -2.0492 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.2638 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab 0.8328 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.7456 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.3368 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK SU-DHL-4 Rituximab -1.2432 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 8.0884 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK RPMI8226 BTZ 8.1379 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK A431 Dasatinib 9.3512 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK RPMI8226 BTZ 9.3392 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK RPMI8226 BTZ 6.4194 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK RPMI8226 BTZ 7.1379 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 8.3313 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 8.4217 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 7.8845 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 8.5487 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 7.3085 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 8.4114 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 7.361 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK RPMI8226 BTZ 7.3853 -
P04637 TP53 P Ser315 ALPNNTSSS(ph)PQPK A431 Imatinib 2 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK A431 Imatinib 8.0062 -
P04637 TP53 P Ser315 RALPNNTSSS(ph)PQPK A431 Dasatinib 5.5031 -

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: