Id: | acc3511 |
Group: | 1sens |
Protein: | p38 MAPK |
Gene Symbol: | MAPK14 |
Protein Id: | Q16539 |
Protein Name: | MK14_HUMAN |
PTM: | phosphorylation |
Site: | Thr180 |
Site Sequence: | LARHTDDEMTGYVATRWYRAP |
Disease Category: | Cancer |
Disease: | Colorectal Cancer |
Disease Subtype: | |
Disease Cellline: | HT-29 |
Disease Info: | |
Drug: | Fisetin + Radiation |
Drug Info: | Fisetin is a natural flavonoid with potential antioxidant and anti - inflammatory properties | Radiation is a physical therapy method often used in cancer treatment to kill cancer cells. |
Relation: |
Fisetin + Radiation
➜
p38 MAPK-Thr180
DOWN
➜
Colorectal Cancer
Alleviate
|
Effect: | suppress |
Effect Info: | Fisetin can enhance the radiosensitivity of human colon cancer HT–29 cells with p53 mutation by downregulating protein phosphorylation. |
Note: | drug comb |
Score: | 4.0 |
Pubmed(PMID): | 20637980 |
Sentence Index: | 20637980_4 |
Sentence: | "Western blot analysis was performed to ascertain the protein levels of gamma-H2AX, phospho-Chk2, active caspase-3, PARP cleavage, phospho-p38, phospho-AKT, and phospho-ERK1/2. RESULTS: Fisetin pretreatment enhanced the radiosensitivity of p53-mutant HT-29 human colorectal cancer cells but not human keratocyte HaCaT cells; it also prolonged radiation-induced G(2)/M arrest, enhanced radiation-induced cell growth arrest in HT-29 cells, and suppressed radiation-induced phospho-H2AX (Ser-139) and phospho-Chk2 (Thr-68) in p53-mutant HT-29 cells. Fisetin could potentially be developed as a novel radiosensitizer against radioresistant human cancer cells." |
Sequence & Structure:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
Select PDB:
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 TargetsPTM Intensity:
source: CPTACMAPK14-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: PTMDResidue | 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: DecryptMNo data.
Function score:
source: funscoRNo data.