Id: acc3350
Group: 2sens
Protein: JNK
Gene Symbol: MAPK8
Protein Id: P45983
Protein Name: MK08_HUMAN
PTM: phosphorylation
Site: Tyr185
Site Sequence: AGTSFMMTPYVVTRYYRAPEV
Disease Category: Cardiovascular and circulatory system diseases
Disease: Endothelial Dysfunction
Disease Subtype: cell apoptosis
Disease Cellline: human umbilical vein endothelial cells (HUVECs)
Disease Info:
Drug: berberine
Drug Info: "Berberine is an isoquinoline alkaloid with various pharmacological properties, commonly used for its potential benefits in treating diarrhea and regulating blood sugar."
Effect: modulate
Effect Info: The drug inhibits JNK phosphorylation and alleviates disease symptoms (apoptosis).
Note:
Score: 4.0
Pubmed(PMID): 27478481
Sentence Index:
Sentence:

Sequence & Structure:

MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MAPK8 BENTAMAPIMOD c-Jun N-terminal kinase, JNK inhibitor 2 Completed endometriosis ClinicalTrials
MAPK8 TANZISERTIB c-Jun N-terminal kinase 1 inhibitor 2 Terminated idiopathic pulmonary fibrosis ClinicalTrials
MAPK8 TANZISERTIB c-Jun N-terminal kinase 1 inhibitor 2 Terminated lupus erythematosus ClinicalTrials
MAPK8 CC-401 c-Jun N-terminal kinase 1 inhibitor 1 Terminated 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
MAPK8-Tyr185
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 185 U Pancreatic cancer Phosphorylation 37016317
Y 185 U Type 2 diabetes Phosphorylation 21931634

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: