Id: acc3879
Group: 1sens
Protein: ERK
Gene Symbol: MAPK3
Protein Id: P27361
Protein Name: MK03_HUMAN
PTM: phosphorylation
Site: Thr202
Site Sequence: PEHDHTGFLTEYVATRWYRAP
Disease Category: Digestive system diseases
Disease: Periodontal Disease
Disease Subtype: "Gingival Inflammation,Periodontal Disease"
Disease Cellline:
Disease Info:
Drug: Orento
Drug Info: "Orento is a drug that may be used for specific medical purposes. However, more detailed information about its functions and indications requires further data. "
Effect: modulate
Effect Info: "Orento inhibits the phosphorylation of ERK, which in turn inhibits the phosphorylation and activation of cPLA2, reduces the production of PGE2, helps relieve gingival inflammation, and improves the condition of periodontal disease."
Note:
Score: 4.0
Pubmed(PMID): 20410594
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
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

PTM-Disease Association:

source: PTMD
Residue 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: DecryptM
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P27361 MAPK3 P Thr202 IADPEHDHTGFLT(ph)EYVATR BT-474 Pertuzumab -1.9738 -
P27361 MAPK3 P Thr202 IADPEHDHTGFLT(ph)EYVATR MDA-MB-175 Trastuzumab -5.405 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: