Id: acc2125
Group: 2sens
Protein: p38
Gene Symbol: MAPK14
Protein Id: Q16539
Protein Name: MK14_HUMAN
PTM: phosphorylation
Site: Thr180
Site Sequence: LARHTDDEMTGYVATRWYRAP
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype: ER+
Disease Cellline: MCF7
Disease Info:
Drug: SB203580
Drug Info: "SB203580 is a selective and ATP-competitive p38 mitogen-activated protein kinase (MAPK) inhibitor with IC50 values of 50 nM for SAPK2a/p38 and 500 nM for SAPK2b/p38beta2, exhibiting lower selectivity against other kinases such as LCK, GSK3beta, and PKBalpha."
Effect: enhance
Effect Info: Treatment with SB203580 or SB202190 enhanced the cellular differentiation and growth inhibition responses induced by RA and caused by p38 phosphorylation.
Note:
Score: 5.0
Pubmed(PMID): 11060298
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-Thr180
Cancer Intensity
BRCA 2.28
COAD 0.452
HGSC -1.055
ccRCC -0.189
GBM -0.187
HNSC 0.188
LUAD 0.929
LUSC 0.063
non_ccRCC -0.898
PDAC -0.317
UCEC -1.265

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 180 P Lung cancer/carcinoma Phosphorylation 22348039
T 180 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: