Id: acc0802
Group: 2sens
Protein: ERK1
Gene Symbol: MAPK3
Protein Id: P27361
Protein Name: MK03_HUMAN
PTM: phosphorylation
Site: Thr202
Site Sequence: PEHDHTGFLTEYVATRWYRAP
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: H1975
Disease Info:
Drug: AZD6244 + BEZ235
Drug Info: "AZD6244: - BEZ235 is a dual ATP-competitive inhibitor of PI3K and mTOR, targeting p110alpha, p110gamma, p110delta, and p110beta with IC50 values of 4, 5, 7, and 75 nM, respectively, and also suppresses mTORC1/2 activity. "
Effect: modulate
Effect Info: "Treatment with AZD6244 or BEZ235 inhibited the phosphorylation of ERK1/2 or AKT, respectively. Combined treatment with AZD6244 and BEZ235 enhanced the inhibition of p-ERK1/2 and p-AKT, and significantly enhanced the anti-tumor effect."
Note: drug comb
Score: 4.0
Pubmed(PMID): 24939055
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: