Id: acc0625
Group: 1sens
Protein: p38MAPK
Gene Symbol: MAPK14
Protein Id: Q16539
Protein Name: MK14_HUMAN
PTM: phosphorylation
Site: Tyr182
Site Sequence: RHTDDEMTGYVATRWYRAPEI
Disease Category: Cancer
Disease: Hepatocellular Carcinoma
Disease Subtype:
Disease Cellline: HepG2
Disease Info:
Drug: sorafenib + berbamine + ouabain
Drug Info: "Sorafenib: Sorafenib is a multikinase inhibitor targeting Raf-1, B-Raf, VEGFR-3, and other kinases, used in the treatment of advanced hepatocellular carcinoma and renal cell carcinoma. Berbamine: Berbamine is a natural bis-benzylisoquinoline alkaloid derived from *Berberis* species, with reported antitumor and immunomodulatory effects. Ouabain: Ouabain is a cardiac glycoside that inhibits the Na?/K?-ATPase pump, historically used to treat specific cardiac conditions like atrial fibrillation and heart failure. "
Effect: modulate
Effect Info: "Sorafenib inhibits the induction of Src, p38MAPK, EGFR, and ERK1/2 phosphorylation by berbamine and ouabain. The combined use of sorafenib with berbamine or ouabain significantly suppresses the viability of sorafenib-resistant cells."
Note: drug comb
Score: 4.0
Pubmed(PMID): 34233013
Sentence Index:
Sentence:

Sequence & Structure:

MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MAPK14 ARRY-797 MAP kinase p38 alpha inhibitor 3 Terminated dilated cardiomyopathy ClinicalTrials
MAPK14 LOSMAPIMOD MAP kinase p38 alpha inhibitor 3 Completed acute coronary syndrome ClinicalTrials
MAPK14 LOSMAPIMOD MAP kinase p38 alpha inhibitor 3 Terminated COVID-19 ClinicalTrials
MAPK14 LOSMAPIMOD MAP kinase p38 alpha inhibitor 3 Active, not recruiting Facioscapulohumeral dystrophy ClinicalTrials
MAPK14 ACUMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed chronic obstructive pulmonary disease ClinicalTrials
ClinicalTrials
MAPK14 SEMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed Crohn's disease ClinicalTrials
ClinicalTrials
ClinicalTrials
MAPK14 PF-03715455 MAP kinase p38 alpha inhibitor 2 Terminated chronic obstructive pulmonary disease ClinicalTrials
MAPK14 DILMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed chronic obstructive pulmonary disease ClinicalTrials
MAPK14 AZD-7624 MAP kinase p38 alpha inhibitor 2 Completed chronic obstructive pulmonary disease ClinicalTrials
MAPK14 SEMAPIMOD MAP kinase p38 alpha inhibitor 2 Terminated Crohn's disease ClinicalTrials
MAPK14 PH-797804 MAP kinase p38 alpha inhibitor 2 Completed chronic obstructive pulmonary disease ClinicalTrials
ClinicalTrials
ClinicalTrials
MAPK14 LOSMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed chronic obstructive pulmonary disease ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
MAPK14 ARRY-797 MAP kinase p38 alpha inhibitor 2 Completed dilated cardiomyopathy ClinicalTrials
ClinicalTrials
MAPK14 DORAMAPIMOD MAP kinase p38 alpha inhibitor 2 Terminated rheumatoid arthritis ClinicalTrials
MAPK14 LOSMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
ClinicalTrials
MAPK14 BMS-582949 MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
MAPK14 DORAMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed psoriasis ClinicalTrials
MAPK14 BMS-582949 MAP kinase p38 alpha inhibitor 2 Completed psoriasis ClinicalTrials
MAPK14 DILMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
ClinicalTrials
MAPK14 PG-760564 MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
MAPK14 TAK-715 MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
MAPK14 TALMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
ClinicalTrials
MAPK14 PH-797804 MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
ClinicalTrials
MAPK14 VX-702 MAP kinase p38 alpha inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
ClinicalTrials
MAPK14 DILMAPIMOD MAP kinase p38 alpha inhibitor 2 Completed coronary artery disease 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
MAPK14-Tyr182
Cancer Intensity
BRCA 2.374
COAD -0.005
HGSC -0.861
ccRCC 0.066
GBM 1.175
HNSC -0.22
LUAD 0.029
LUSC -0.105
non_ccRCC -0.927
PDAC -0.488
UCEC -1.039

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 182 D Breast cancer/tumor/carcinoma Phosphorylation 23771849
Y 182 U Bladder cancer Phosphorylation 33204153

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: