Id: acc1686
Group: 2sens
Protein: ERK2
Gene Symbol: MAPK1
Protein Id: P28482
Protein Name: MK01_HUMAN
PTM: phosphorylation
Site: Tyr187
Site Sequence: HDHTGFLTEYVATRWYRAPEI
Disease Category: Cancer
Disease: Glioma
Disease Subtype:
Disease Cellline: C6
Disease Info:
Drug: temozolomide(TMZ)
Drug Info: "Temozolomide (TMZ) is an alkylating chemotherapeutic agent primarily used in the treatment of glioblastoma multiforme, functioning by inhibiting DNA synthesis in cancer cells through methylation of guanine residues, and is often administered in combination with radiotherapy."
Effect: modulate
Effect Info: TMZ reduces protein phosphorylation and inhibits tumors.
Note:
Score: 4.0
Pubmed(PMID): 27878252
Sentence Index:
Sentence:

Sequence & Structure:

MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 2 Terminated neoplasm ClinicalTrials
MAPK1 TEMUTERKIB Mitogen-activated protein kinase; ERK1/ERK2 inhibitor 2 Completed pancreatic carcinoma ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 2 Recruiting histiocytic neoplasm ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 2 Active, not recruiting Uveal Melanoma ClinicalTrials
MAPK1 TEMUTERKIB Mitogen-activated protein kinase; ERK1/ERK2 inhibitor 2 Terminated cancer ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 1 Completed acute myeloid leukemia ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 1 Completed myelodysplastic syndrome ClinicalTrials
MAPK1 TEMUTERKIB Mitogen-activated protein kinase; ERK1/ERK2 inhibitor 1 Recruiting acute myeloid leukemia ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 1 Completed neoplasm ClinicalTrials
ClinicalTrials
MAPK1 MK-8353 MAP kinase ERK2 inhibitor 1 Completed neoplasm ClinicalTrials
MAPK1 RAVOXERTINIB MAP kinase ERK2 inhibitor 1 Completed neoplasm ClinicalTrials
MAPK1 MK-8353 MAP kinase ERK2 inhibitor 1 Terminated neoplasm ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 1 Recruiting pancreatic carcinoma ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 1 Terminated pancreatic carcinoma ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 inhibitor 1 Recruiting metastatic colorectal cancer ClinicalTrials
MAPK1 KO-947 Mitogen-activated protein kinase; ERK1/ERK2 inhibitor 1 Terminated cancer ClinicalTrials
MAPK1 MK-8353 MAP kinase ERK2 inhibitor 1 Completed colorectal cancer ClinicalTrials
MAPK1 TEMUTERKIB Mitogen-activated protein kinase; ERK1/ERK2 inhibitor 0.5 Recruiting glioblastoma multiforme ClinicalTrials
MAPK1 ULIXERTINIB MAP kinase ERK2 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
MAPK1-Tyr187
Cancer Intensity
BRCA 0.772
COAD 0.273
HGSC 0.701
ccRCC -0.806
GBM 0.279
HNSC 0.328
LUAD 0.387
LUSC 0.866
non_ccRCC -2.593
PDAC 0.32
UCEC -0.527

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 187 U Thyroid cancer/carcinoma Phosphorylation 17209045
Y 187 U Triple-negative breast cancer Phosphorylation 28415597

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
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR A431 Imatinib 5.4775 up
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR BT-474 Lapatinib 6.6172 down
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR K562 Dasatinib 8.8776 down
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR KYSE-520 SHP099 6.2002 down
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR MDA-MB-175 Lapatinib 7.3646 down
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR MDA-MB-175 Pertuzumab -4.632 down
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR PC-9 LapatinibAZD4547 6.4194 down
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR PC-9 Lapatinib 6.4558 down
P28482 MAPK1 P Thr185;Tyr187 VADPDHDHTGFLT(ph)EY(ph)VATR SK-BR-3 Trastuzumab -1.2287 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR A431 Dasatinib 6.1777 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR SK-BR-3 Trastuzumab -0.81 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR SK-BR-3 Pertuzumab -1.7704 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR SK-BR-3 Lapatinib 4.7218 -
P28482 MAPK1 P Tyr187;Thr190 VADPDHDHTGFLTEY(ph)VAT(ph)R PC-9 AZD4547 1.938 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR PC-9 AZD4547 7.196 -
P28482 MAPK1 P Thr185;Tyr187 VADPDHDHTGFLT(ph)EY(ph)VATR PC-9 AZD4547 7.2923 -
P28482 MAPK1 P Thr185;Tyr187 VADPDHDHTGFLT(ph)EY(ph)VATR MDA-MB-175 Trastuzumab -1.6811 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR MDA-MB-175 Trastuzumab 5 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR K562 Imatinib 7.13 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR BT-474 Trastuzumab -2.1745 -
P28482 MAPK1 P Tyr187 VADPDHDHTGFLTEY(ph)VATR BT-474 Pertuzumab -1.9633 -

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: