MAP2K2

(redirected from MEK2)

MAP2K2

A gene on chromosome 19p13.3 that encodes mitogen-activated protein kinase kinase 2, which catalyses the simultaneous phosphorylation of a threonine and a tyrosine residue in MAP kinases; it also activates the ERK1 and ERK2 MAP kinases.

Molecular pathology
Defects of MAP2K2 cause cardiofaciocutaneous syndrome.
References in periodicals archive ?
12) Some of these mutations, such as MEK1 P124 (substitution of proline at position 124), MEK1 C121S (serine for cysteine substitution at position 121), and MEK2 C125S (serine for cysteine substitution at position 125), are particularly concerning because they might confer resistance to targeted drugs.
MEK inhibitor-induced receptor tyrosine kinase (RTK) stimulation overcame MEK2 inhibition, reactivating ERK and resulting in drug resistance.
Zhang H, Feng H, Luo L, Zhou Q, Luo Z, Peng Y (2010) Distinct effects of knocking down MEK1 and MEK2 on replication of herpes simplex virus type 2.
Trametinib, a reversible inhibitor of MEK1 and MEK2, is reportedly approved by the US FDA under the name Mekinist for the treatment of adult patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutation as detected by an FDA-approved test.
Implication of MEK1 and MEK2 in the establishment of the blood-placenta barrier during placentogenesis in mouse.
Meanwhile, MAPK signaling pathway molecules including MEKK1, ASK1 (MAP3K5), MLK2 (MAP3K10), MLK3, NIK, MEK1 (MAP2K1), MEK2 (MAP2K2), MEK4 (MAP2K4), MEK7 (MAP2K7), ERK1 (MAPK3), JNK1 (MAPK8) and JNK2 (MAPK9) were significantly up-regulated and revealed 2.
By selectively inhibiting MEK1 and MEK2, U0126 signal transduction agent functionally antagonizes AP1-mediated transcriptional activation.
Trametinib (GSK1120212) is also an investigational, orally bioavailable inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2.
RAF phosphorylates and activates both MEK1 and MEK2 on two distinct serine residues (Crews et al.
MEK162, a small molecule selective inhibitor of the kinases MEK1 and MEK2, showed clinical activity and good tolerability in this patient population.
NCCN recently received $4 million in the form of two research grants from GlaxoSmithKline to gain further insights into GSK2118436, a BRAF inhibitor, and GSK1120212, a MEK1 and MEK2 inhibitor, both promising therapies in the treatment of advanced melanoma.