Id: acc1106
Group: 2sens
Protein: MEK2
Gene Symbol: MAP2K2
Protein Id: P36507
Protein Name: MP2K2_HUMAN
PTM: phosphorylation
Site: Ser222
Site Sequence: FGVSGQLIDSMANSFVGTRSY
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: H1975
Disease Info:
Drug: gefitinib + Lovastatin
Drug Info: Gefitinib: - Lovastatin: Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
Effect: modulate
Effect Info: "Lovastatin inhibits cholesterol synthesis and makes gefitinib - resistant cell lines sensitive to gefitinib. The combined use has a significant inhibitory effect on the phosphorylation of EGFR, Akt - 1, MEK1/2, and ERK1/2."
Note: drug comb
Score: 4.0
Pubmed(PMID): 29215723
Sentence Index:
Sentence:

Sequence & Structure:

MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADLKMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MAP2K2 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - neoplasm ATC
MAP2K2 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 4 - neoplasm ATC
MAP2K2 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - neoplasm ATC
MAP2K2 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 Recruiting neoplasm ClinicalTrials
MAP2K2 COBIMETINIB FUMARATE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - melanoma EMA
MAP2K2 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - melanoma DailyMed
EMA
MAP2K2 COBIMETINIB FUMARATE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - metastatic melanoma DailyMed
MAP2K2 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - metastatic melanoma FDA
MAP2K2 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - metastatic melanoma FDA
MAP2K2 SELUMETINIB SULFATE Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 4 - neurofibromatosis DailyMed
MAP2K2 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - thyroid cancer DailyMed
MAP2K2 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 - lung cancer DailyMed
MAP2K2 SELUMETINIB SULFATE Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 4 - neurofibromatosis type 1 FDA
EMA
MAP2K2 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Recruiting astrocytoma ClinicalTrials
MAP2K2 SELUMETINIB SULFATE Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Recruiting astrocytoma ClinicalTrials
MAP2K2 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Completed cutaneous melanoma ClinicalTrials
MAP2K2 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Active, not recruiting melanoma ClinicalTrials
MAP2K2 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Completed melanoma ClinicalTrials
MAP2K2 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Terminated melanoma ClinicalTrials
MAP2K2 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Withdrawn melanoma ClinicalTrials
MAP2K2 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Active, not recruiting melanoma ClinicalTrials
ClinicalTrials
ClinicalTrials
MAP2K2 TRAMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Recruiting melanoma ClinicalTrials
ClinicalTrials
MAP2K2 TRAMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Active, not recruiting melanoma ClinicalTrials
MAP2K2 TRAMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Completed melanoma ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
MAP2K2 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Active, not recruiting non-small cell lung carcinoma 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
MAP2K2-Ser222
Cancer Intensity
BRCA 1.103
COAD 0.207
HGSC -2.178
ccRCC -0.277
GBM -0.734
HNSC 1.342
LUAD 0.555
LUSC 0.176
non_ccRCC -0.246
PDAC -0.741
UCEC 0.793

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 394 U Breast cancer Phosphorylation 33226073
- - U Breast cancer Phosphorylation 15193230
K 48 U Hepatocellular carcinoma Ubiquitination 29706623

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: