Id: | acc4923 |
Group: | 1sens |
Protein: | ERK2 |
Gene Symbol: | Mapk1 |
Protein Id: | P63086 |
Protein Name: | MK01_RAT |
PTM: | phosphorylation |
Site: | Tyr187 |
Site Sequence: | HTGFLTEYVATRWYRAPEIML |
Disease Category: | Cardiovascular and circulatory system diseases |
Disease: | Pulmonary Artery Proliferation |
Disease Subtype: | 5-HT induced |
Disease Cellline: | |
Disease Info: | |
Drug: | KMUP-1 |
Drug Info: | KMUP-1 is a novel drug with potential effects in cardiovascular protection and anti - inflammatory activities. It has been investigated for its possible therapeutic applications in relevant pathological conditions. |
Effect: | modulate |
Effect Info: | "KMUP-1 inhibits MCT-induced pulmonary artery hyperplasia by binding to 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptors, increasing the expression of endothelial cell eNOS/5-HT(2B) receptors and NO release, and inhibiting the expression of 5-HTT/RhoA/ROCK and the phosphorylation of AKT/ERK. KMUP-1 is promising for the treatment of 5-HT-induced pulmonary artery hyperplasia." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 20870034 |
Sentence Index: | 20870034_1 |
Sentence: | "KMUP-1 inhibits monocrotaline (MCT)-induced pulmonary artery (PA) proliferation by targeting serotonin (5-HT) receptors, inactivating RhoA and reducing phosphorylation of AKT/ERK." |
Sequence & Structure:
MAAAAAAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNLNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
Select PDB:
No data.
Protein Tractability:
source: Open TargetsNo data.
PTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
- | - | A | Basophilic leukemia | Phosphorylation | 11971018 |
T | 183 | D | Major depressive disorder | Phosphorylation | 16959794 |
Y | 185 | D | Major depressive disorder | Phosphorylation | 16959794 |
T | 183 | U | Uteroplacental insufficiency | Phosphorylation | 16940436 |
Y | 185 | U | Uteroplacental insufficiency | Phosphorylation | 16940436 |
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.