2015年9月24日 · New drugs that inhibit RAF or MEK1 and MEK2 have recently been approved or are currently undergoing late-stage clinical evaluation. In this Review, we consider the ERK pathway, focusing...

Dual specificity mitogen-activated protein kinase kinase 2 is an enzyme that in humans is encoded by the MAP2K2 gene. [5] . It is more commonly known as MEK2, but has many alternative names including CFC4, MKK2, MAPKK2 and PRKMK2. [6] The protein encoded by this gene is a dual specificity protein kinase that belongs to the MAP kinase kinase family.

2004年11月14日 · Here we present the X-ray structures of human MEK1 and MEK2, each determined as a ternary complex with MgATP and an inhibitor to a resolution of 2.4 Å and 3.2 Å, respectively. The structures...

2012年1月6日 · MEK1 and MEK2 are related protein kinases that participate in the RAS-RAF-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes including apoptosis, cell cycle progression, cell migration, differentiation, metabolism, and proliferation.

Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma.

New drugs that inhibit RAF or MEK1 and MEK2 have recently been approved or are currently undergoing late-stage clinical evaluation. In this Review, we consider the ERK pathway, focusing particularly on the role of MEK1 and MEK2, the 'gatekeepers' of ERK1/2 activity.

This demonstrates the pivotal roles of MEK1/2 in malignant transformation, rationalizing therapeutic targeting of upregulated MEK1/2 activity in cancer. In addition, there are unique characteristics of MEK1 and MEK2 that might support the advantage of therapeutic development of MEK1/2 inhibition.

MEK2 is a critical modulating mechanism to down-regulate GCIP stability and function in cancer cells. USP21-mediated deubiquitination and stabilization of MEK2 plays a critical role in hepatocellular carcinoma development.

2012年1月6日 · MEK1/2 are dual-specificity protein kinases that mediate the phosphorylation of tyrosine and then threonine in ERK1 or ERK2, their only known physiological substrates. This phosphorylation activates ERK1/2, which are protein-serine/threonine kinases.

2014年5月20日 · Highly selective and potent non-ATP-competitive allosteric MEK1/2 inhibitors have been developed and assessed in numerous clinical studies over the past decade.