Article
Macrocyclic MEK1/2 inhibitor with efficacy in a mouse model of cardiomyopathy caused by lamin A/C gene mutation.
Bioorganic & medicinal chemistry - 1 Feb 2017
Wu Wei, Chordia Mahendra D, Hart Barry P, Kumarasinghe E Sathyajith, Ji Min K, Bhargava Ajay, Lawlor Michael W, Shin Ji-Yeon, Sera Fusako, Homma Shunichi, Muchir Antoine, Khire Uday R, Worman Howard J
Abstract excerpt
Signaling mediated by extracellular signal-regulated kinases 1 and 2 (ERK1/2) is involved in numerous cellular processes. Mitogen-activated protein kinase kinases (MEK1/2) catalyze the phosphorylation of ERK1/2, converting it into an active kinase that regulates the expression of numerous genes and cellular processes. Inhibitors of MEK1/2 have demonstrated preclinical and clinical efficacy in certain cancers and...
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