Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766, That Suppresses Feedback Reactivation of RAF Activity [Image: see text]

Tumors with mutant RAS are often dependent on extracellular signal–regulated kinase (ERK) signaling for growth; however, MEK inhibitors have only marginal antitumor activity in these tumors. MEK inhibitors relieve ERK-dependent feedback inhibition of RAF and cause induction of MEK phosphorylation. W...

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Hauptverfasser: Ishii, Nobuya, Harada, Naoki, Joseph, Eric W., Ohara, Kazuhiro, Miura, Takaaki, Sakamoto, Hiroshi, Matsuda, Yutaka, Tomii, Yasushi, Tachibana-Kondo, Yukako, Iikura, Hitoshi, Aoki, Toshihiro, Shimma, Nobuo, Arisawa, Mikio, Sowa, Yoshihiro, Poulikakos, Poulikos I., Rosen, Neal, Aoki, Yuko, Sakai, Toshiyuki
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2013
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4115369/
https://ncbi.nlm.nih.gov/pubmed/23667175
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1158/0008-5472.CAN-12-3937
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