Id: acc1115
Group: 2sens
Protein: MEK1
Gene Symbol: MAP2K1
Protein Id: Q02750
Protein Name: MP2K1_HUMAN
PTM: phosphorylation
Site: Ser221
Site Sequence: SGQLIDSMANSFVGTRSYMSP
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: PC-9/GR
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, making the 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:

MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MAP2K1 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - neoplasm ATC
MAP2K1 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 4 - neoplasm ATC
MAP2K1 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - neoplasm ATC
MAP2K1 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 Recruiting neoplasm ClinicalTrials
MAP2K1 COBIMETINIB FUMARATE Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - melanoma EMA
MAP2K1 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - melanoma DailyMed
EMA
MAP2K1 COBIMETINIB FUMARATE Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - metastatic melanoma DailyMed
MAP2K1 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - metastatic melanoma FDA
MAP2K1 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - metastatic melanoma FDA
MAP2K1 SELUMETINIB SULFATE Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 4 - neurofibromatosis DailyMed
MAP2K1 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - thyroid cancer DailyMed
MAP2K1 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 - lung cancer DailyMed
MAP2K1 SELUMETINIB SULFATE Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 4 - neurofibromatosis type 1 EMA
FDA
MAP2K1 SELUMETINIB SULFATE Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Recruiting astrocytoma ClinicalTrials
MAP2K1 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Recruiting astrocytoma ClinicalTrials
MAP2K1 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Completed cutaneous melanoma ClinicalTrials
MAP2K1 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Withdrawn melanoma ClinicalTrials
MAP2K1 TRAMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Recruiting melanoma ClinicalTrials
ClinicalTrials
MAP2K1 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Active, not recruiting melanoma ClinicalTrials
MAP2K1 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Completed melanoma ClinicalTrials
MAP2K1 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Terminated melanoma ClinicalTrials
MAP2K1 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Active, not recruiting melanoma ClinicalTrials
ClinicalTrials
ClinicalTrials
MAP2K1 TRAMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Active, not recruiting melanoma ClinicalTrials
MAP2K1 TRAMETINIB Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor 3 Completed melanoma ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
MAP2K1 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

No intensity data of this site,
show all other sites!

MAP2K1-Ser212
Cancer Intensity
BRCA
COAD 0.336
HGSC -2.466
ccRCC
GBM 0.491
HNSC 0.463
LUAD 0.347
LUSC 0.32
non_ccRCC 0.267
PDAC
UCEC 0.243
MAP2K1-Ser218
Cancer Intensity
BRCA 1.025
COAD 0.17
HGSC -2.102
ccRCC
GBM -0.726
HNSC 1.253
LUAD 0.502
LUSC 0.141
non_ccRCC -0.26
PDAC -0.732
UCEC 0.729
MAP2K1-Ser222
Cancer Intensity
BRCA 1.754
COAD -0.057
HGSC -2.024
ccRCC
GBM 0.263
HNSC 0.783
LUAD 0.076
LUSC 0.656
non_ccRCC -0.519
PDAC -0.44
UCEC -0.492
MAP2K1-Thr286
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM 1.485
HNSC -0.682
LUAD -0.348
LUSC -0.455
non_ccRCC
PDAC
UCEC
MAP2K1-Thr7
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD -1.121
LUSC
non_ccRCC
PDAC 0.32
UCEC 0.801

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - P Colon cancer/carcinoma Phosphorylation 15233637
- - P Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 24209743
S 218 U Head and neck squamous cell carcinoma Phosphorylation 21281788
S 222 U Head and neck squamous cell carcinoma Phosphorylation 21281788
- - U Breast cancer Phosphorylation 15193230
- - U Crohn's disease Phosphorylation 23970928
- - U Adenoma Phosphorylation 21989899

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: