Id: acc1511
Group: 2sens
Protein: ERK
Gene Symbol: MAPK3
Protein Id: P27361
Protein Name: MK03_HUMAN
PTM: phosphorylation
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Bladder Cancer
Disease Subtype:
Disease Cellline: J82
Disease Info:
Drug: sorafenib
Drug Info: "Sorafenib is a multikinase inhibitor that targets Raf kinases, vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptor (PDGFR), and other kinases, primarily used in the treatment of advanced renal cell carcinoma, unresectable hepatocellular carcinoma, and radioactive iodine-refractory differentiated thyroid cancer."
Effect: modulate
Effect Info: "At pharmacological concentrations (≥3 μM), the inhibitory effects of sorafenib on ERK - 1/2 phosphorylation, migration, and proliferation, as well as its pro - apoptotic effect."
Note:
Score: 4.0
Pubmed(PMID): 20649572
Sentence Index:
Sentence:

Sequence & Structure:

MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAYDHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYIVQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDLKICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSDSKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERLKELIFQETARFQPGVLEAP

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

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 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

No 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: PTMD
Residue Position State Disease Class PMID
- - A Non-small cell lung cancer Phosphorylation 36966223
- - A Recessive parkinson disease Phosphorylation 23261939
- - A Colon cancer/carcinoma Phosphorylation 23786838
- - D Colorectal cancer Phosphorylation 36526622
- - P Colon cancer/carcinoma Phosphorylation 23183114
- - P Colon cancer/carcinoma Phosphorylation 24085800
- - P Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 24209743
- - P Liver cancer Phosphorylation 23693078
- - P Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 9927031
- - P Myeloma Phosphorylation 11986233
- - P Non-small cell lung cancer/carcinoma Phosphorylation 24096476
- - P Bladder cancer Phosphorylation 24375195
- - P Non-small cell lung cancer/carcinoma Phosphorylation 23306155
- - U Adenoma Phosphorylation 21989899
- - U Breast cancer/tumor/carcinoma Phosphorylation 24374773
- - U Lung cancer/carcinoma Phosphorylation 24286320
- - U Bipolar disorder Phosphorylation 24075327
- - U Crohn's disease Phosphorylation 23970928
- - U Lung cancer Phosphorylation 34439211
- - U Breast cancer Phosphorylation 15193230
- - U Ovarian cancer/carcinoma Phosphorylation 14961570
- - U Pancreatic cancer Phosphorylation 21678462
- - U Glioblastoma Phosphorylation 36493392
- - U Clear cell renal cell carcinoma Phosphorylation 37454877
- - U Osteosarcoma Phosphorylation 31383289
- - U Lymphoma Phosphorylation 23620775
- - U Ovarian cancer/carcinoma Phosphorylation 23285101

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: