Id: acc1673
Group: 2sens
Protein: ERK
Gene Symbol: MAPK3
Protein Id: P27361
Protein Name: MK03_HUMAN
PTM: phosphorylation
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Thyroid Cancer
Disease Subtype:
Disease Cellline:
Disease Info:
Drug: apigenin
Drug Info: "Apigenin is a naturally occurring flavonoid compound with demonstrated potential as an antifungal agent in the preparation of drugs against human fungal infections, and it is also being researched in drug delivery systems such as solid lipid nanoparticles (APG-SLNP) to enhance stability and bioavailability. "
Effect: modulate
Effect Info: Apigenin inhibits the growth of thyroid cancer cells by suppressing the tyrosine phosphorylation of epidermal growth factor receptor (EGF-R) and the phosphorylation of ERK mitogen-activated protein (MAP) kinase.
Note:
Score: 4.0
Pubmed(PMID): 11299771
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: