Id: acc2036
Group: 2sens
Protein: MEK2
Gene Symbol: MAP2K2
Protein Id: P36507
Protein Name: MP2K2_HUMAN
PTM: phosphorylation
Site: Ser217
Site Sequence: IKLCDFGVSGQLIDSMANSFV
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype:
Disease Cellline: SK-BR-3
Disease Info:
Drug: DHA
Drug Info: -
Effect: modulate
Effect Info: DHA induces apoptosis in human breast cancer cells (MCF-7 and SK-BR-3) and mouse mammary gland tissue by inhibiting the action of SDC - 1 in the MEK - Erk signaling pathway.
Note:
Score: 4.0
Pubmed(PMID): 21771724
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

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

MAP2K2-Ser216
Cancer Intensity
BRCA
COAD 0.332
HGSC -2.654
ccRCC 0.205
GBM 0.498
HNSC 0.468
LUAD 0.344
LUSC 0.315
non_ccRCC 0.259
PDAC
UCEC 0.233
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
MAP2K2-Ser226
Cancer Intensity
BRCA 1.866
COAD -0.038
HGSC -2.106
ccRCC -0.217
GBM 0.298
HNSC 0.845
LUAD 0.102
LUSC 0.712
non_ccRCC -0.524
PDAC -0.441
UCEC -0.496
MAP2K2-Ser23
Cancer Intensity
BRCA
COAD -0.187
HGSC -1.963
ccRCC 0.835
GBM 0.513
HNSC 0.273
LUAD
LUSC
non_ccRCC 0.949
PDAC -0.419
UCEC
MAP2K2-Ser26
Cancer Intensity
BRCA
COAD -0.238
HGSC
ccRCC 1.223
GBM -1.454
HNSC -0.101
LUAD 0.57
LUSC
non_ccRCC
PDAC
UCEC
MAP2K2-Ser30
Cancer Intensity
BRCA
COAD 0.707
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC -0.707
UCEC
MAP2K2-Ser76
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.895
GBM -1.08
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.185
MAP2K2-Thr17
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -0.707
GBM
HNSC
LUAD 0.707
LUSC
non_ccRCC
PDAC
UCEC
MAP2K2-Thr25
Cancer Intensity
BRCA
COAD -0.451
HGSC
ccRCC 0.234
GBM 1.524
HNSC -1.184
LUAD -0.123
LUSC
non_ccRCC
PDAC
UCEC
MAP2K2-Thr394
Cancer Intensity
BRCA -0.026
COAD
HGSC 2.485
ccRCC -0.291
GBM -0.696
HNSC 0.064
LUAD 0.242
LUSC 0.231
non_ccRCC -0.063
PDAC -0.625
UCEC -1.321
MAP2K2-Thr396
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

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: