Id: acc3738
Group: 1sens
Protein: ERK2
Gene Symbol: MAPK1
Protein Id: P28482
Protein Name: MK01_HUMAN
PTM: phosphorylation
Site: Tyr187
Site Sequence: HDHTGFLTEYVATRWYRAPEI
Disease Category: Cancer
Disease: Pancreatic Cancer
Disease Subtype:
Disease Cellline: PK - 1
Disease Info:
Drug: U0126
Drug Info: "U0126 is a drug, but specific details about it are not provided."
Effect: modulate
Effect Info: "The specific MEK inhibitors PD98059/U0126 inhibit the growth of human pancreatic cancer cells by suppressing the phosphorylation of ERK1/2, suggesting that the drugs exert their anti - tumor effects by regulating the phosphorylation modification of ERK1/2."
Note:
Score: 4.0
Pubmed(PMID): 15896303
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: