Molecule Details

General Information of the Molecule

Name

ERK activator kinase 2 (MEK2)

Synonyms

PRKMK2; MKK2; MEK 2; MAPKK 2; MAPK/ERK kinase 2; MAP kinase kinase 2; Dual specificity mitogenactivated protein kinase kinase 2; Dual specificity mitogen-activated protein kinase kinase 2

Gene Name

MAP2K2

Gene ID

5605

Sequence

MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQ
KAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQ
VLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRG
LAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQ
GTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRP
PGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADL
KMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV

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Function

Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases (By similarity). Activates BRAF in a KSR1 or KSR2-dependent manner; by binding to KSR1 or KSR2 releases the inhibitory intramolecular interaction between KSR1 or KSR2 protein kinase and N-terminal domains which promotes KSR1 or KSR2-BRAF dimerization and BRAF activation.

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Uniprot ID

MP2K2_HUMAN

EC Number

EC: 2.7.12.2

Pfam

PF00069

KEGG ID

hsa5605

TTD ID

T89055

A List of Drug Combination(s) Able to Regulate This Molecule

Expression Regulation

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Down-regulation

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Drug Combination 1 Down-regulating the Expression of This Molecule

[1]

Detail(s)

Combination Info

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Name

Arsenic trioxide NP Info

Sorafenib Drug Info

Structure

Phosphorylation Regulation

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Down-regulation

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Drug Combination 1 Down-regulating the Phosphorylation of This Molecule

[2]

Detail(s)

Combination Info

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Name

Fisetin NP Info

Sorafenib Drug Info

Structure

Drug Combination 2 Down-regulating the Phosphorylation of This Molecule

[3]

Detail(s)

Combination Info

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Name

Curcumin NP Info

Gefitinib Drug Info

Structure

Drug(s) of This Target

Selumetinib

Drug Info

Phase 3

Melanoma

References

Reference 1

[Inhibitory effect of sorafenib combined with arsenic trioxide on hepatocellular carcinoma cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2008 Apr;28(4):639-41.

Reference 2

Fisetin, a phytochemical, potentiates sorafenib-induced apoptosis and abrogates tumor growth in athymic nude mice implanted with BRAF-mutated melanoma cells. Oncotarget. 2015 Sep 29;6(29):28296-311.

Reference 3

Curcumin overcome primary gefitinib resistance in non-small-cell lung cancer cells through inducing autophagy-related cell death. J Exp Clin Cancer Res. 2019 Jun 13;38(1):254.

Reference 4

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

Molecule Details

Cite NPCDR

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xinbing SUI (hzzju@hznu.edu.cn)