Id: | acc3535 |
Group: | 2sens |
Protein: | ERK |
Gene Symbol: | MAPK3 |
Protein Id: | P27361 |
Protein Name: | MK03_HUMAN |
PTM: | phosphorylation |
Site: | Thr202/Tyr204 |
Site Sequence: | PEHDHTGFLTEYVATRWYRAP |
Disease Category: | Cancer |
Disease: | Hemangioma |
Disease Subtype: | Infantile Hemangiomas |
Disease Cellline: | HUVECs |
Disease Info: | |
Drug: | Propranolol |
Drug Info: | "Propranolol is a beta - blocker used to treat high blood pressure, irregular heart rhythms, and other heart - related conditions." |
Effect: | modulate |
Effect Info: | "The drug inhibits phosphorylated signaling proteins, indicating that it achieves the therapeutic effect on IHs by inhibiting the angiogenesis signaling pathway mediated by VEGF." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 33575332 |
Sentence Index: | 33575332_8-9 |
Sentence: | "Further studies showed that it could not only inhibit the migration, invasion, and tube formation ability of HUVECs after VEGF induction but also inhibit the phosphorylated protein expressions of angiogenesis-related signaling molecules like AKT, mTOR, ERK, and FAK in HUVECs, with a concentration-dependent inhibitory effect. Conclusion: Propranolol can inhibit the proliferation, migration, invasion, adhesion, and tube formation of hemangioma endothelial cells; block VEGF-mediated angiogenesis signaling pathway; suppress the expressions of downstream angiogenesis-related signaling molecules; and ultimately achieve the effect of treatment of IHs." |
Sequence & Structure:
MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAYDHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYIVQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDLKICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSDSKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERLKELIFQETARFQPGVLEAP
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 2 | Terminated | neoplasm | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 2 | Completed | pancreatic carcinoma | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 2 | Recruiting | histiocytic neoplasm | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 2 | Active, not recruiting | Uveal Melanoma | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 2 | Terminated | cancer | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | acute myeloid leukemia | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | myelodysplastic syndrome | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 1 | Recruiting | acute myeloid leukemia | ClinicalTrials |
MAPK3 | RAVOXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | neoplasm | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | neoplasm | ClinicalTrials ClinicalTrials |
MAPK3 | MK-8353 | MAP kinase ERK1 inhibitor | 1 | Completed | neoplasm | ClinicalTrials |
MAPK3 | MK-8353 | MAP kinase ERK1 inhibitor | 1 | Terminated | neoplasm | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Recruiting | pancreatic carcinoma | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Terminated | pancreatic carcinoma | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Recruiting | metastatic colorectal cancer | ClinicalTrials |
MAPK3 | KO-947 | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 1 | Terminated | cancer | ClinicalTrials |
MAPK3 | MK-8353 | MAP kinase ERK1 inhibitor | 1 | Completed | colorectal cancer | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 0.5 | Recruiting | glioblastoma multiforme | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 0.5 | Recruiting | Paraganglioma | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo intensity data of this site,
show all other sites!
MAPK3-Thr198 | |||||
---|---|---|---|---|---|
Cancer | Intensity | ||||
BRCA | |||||
COAD | 1.198 | ||||
HGSC | -0.815 | ||||
ccRCC | 0.207 | ||||
GBM | 0.819 | ||||
HNSC | 0.415 | ||||
LUAD | -0.091 | ||||
LUSC | |||||
non_ccRCC | |||||
PDAC | |||||
UCEC | -1.734 |
MAPK3-Thr202 | |||||
---|---|---|---|---|---|
Cancer | Intensity | ||||
BRCA | 2.637 | ||||
COAD | -0.058 | ||||
HGSC | 0.315 | ||||
ccRCC | -0.838 | ||||
GBM | -0.198 | ||||
HNSC | -0.165 | ||||
LUAD | 0 | ||||
LUSC | 0.376 | ||||
non_ccRCC | -1.222 | ||||
PDAC | -0.124 | ||||
UCEC | -0.724 |
MAPK3-Tyr204 | |
---|---|
Cancer | Intensity |
BRCA | 1.299 |
COAD | 0.294 |
HGSC | 1.686 |
ccRCC | -0.456 |
GBM | 0.155 |
HNSC | 0.082 |
LUAD | -0.027 |
LUSC | 0.328 |
non_ccRCC | -0.355 |
PDAC | -1.055 |
UCEC | -1.949 |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
T | 202 | D | Acute lymphocytic leukemia | Phosphorylation | 26073130 |
T | 202 | D | Head and neck squamous cell carcinoma | Phosphorylation | 21281788 |
T | 202 | U | Pulmonary emphysema | Phosphorylation | 14764579 |
T | 202 | U | Acute myelogenous leukemia | Phosphorylation | 26073130 |
T | 202 | U | Alzheimer's disease | Phosphorylation | 35847683 |
T | 202 | U | Glioma | Phosphorylation | 33820494 |
T | 202 | U | Breast cancer | Phosphorylation | 31944568 |
T | 202 | U | Hepatocellular carcinoma | Phosphorylation | 36230524 |
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.