What is MEK1 and MEK2?

MEK1 and MEK2 are dual-specificity kinases that activate ERK1 and ERK2 by phosphorylating them at conserved threonine and tyrosine residues in the T-E-Y motif found in their activation loop.

What does MEK1 stand for?

Mitogen-activated protein kinase kinase

What does MAPK pathway do?

MAPK pathways relay, amplify and integrate signals from a diverse range of stimuli and elicit an appropriate physiological response including cellular proliferation, differentiation, development, inflammatory responses and apoptosis in mammalian cells.

What is RAS and RAF?

Ras is a type of small GTP-binding protein. Raf, a serine/threonine protein kinase, can phosphorylate proteins directly or promote protein phosphorylation via MEK/ERK activation downstream and regulate the apoptotic process.

How are MEK1 and MEK2 kinases related?

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition MEK1 and MEK2 are closely related, dual-specificity tyrosine/threonine protein kinases found in the Ras/Raf/MEK/ERK mitogen-activated protein kinase (MAPK) signaling pathway.

Which is part of the MAPK / ERK pathway?

MAPK/ERK pathway. The pathway includes many proteins, including MAPK ( mitogen-activated protein kinases, also called ERK, extracellular signal-regulated kinases ), [citation needed] which communicate by adding phosphate groups to a neighboring protein, which acts as an “on” or “off” switch.

Which is an activator of the RAF / MEK / ERK pathway?

Ras—an upstream activator of the Raf/MEK/ERK kinase cascade. Ras is a small GTP-binding protein, which is the common upstream molecule of several signaling pathways including Raf/MEK/ERK, PI3K/Akt and RalEGF/Ral [3]. Four Ras proteins have been identified, namely Ha-Ras, N-Ras, Ki-Ras 4A and Ki-Ras 4B.

Are there any first generation MEK1 / 2 inhibitors?

Second, it helps understand why the first-generation MEK1/2 inhibitors PD98059, U0126 and PD184352 were also found to inhibit MEK5 and the ERK5 MAP kinase pathway at higher concentrations [ 17, 18 ].