Dataset Information


Homo sapiens

ABSTRACT: Antitumor efficacy of RAF inhibitor GDC-0879 involving BRAFV600E mutational status and ERK/MAPK pathway suppression

ORGANISM(S): Homo sapiens  



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Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.

Hoeflich Klaus P KP   Herter Sylvia S   Tien Janet J   Wong Leo L   Berry Leanne L   Chan Jocelyn J   O'Brien Carol C   Modrusan Zora Z   Seshagiri Somasekar S   Lackner Mark M   Stern Howard H   Choo Edna E   Murray Lesley L   Friedman Lori S LS   Belvin Marcia M  

Cancer research 20090310 7

Oncogenic activation of the BRAF serine/threonine kinase has been associated with initiation and maintenance of melanoma tumors. As such, development of pharmacologic agents to target RAF proteins or their effector kinases is an area of intense investigation. Here we report the biological properties of GDC-0879, a highly selective, potent, and orally bioavailable RAF small-molecule inhibitor. We used extracellular signal-regulated kinase (ERK)-1/2 and mitogen-activated protein kinase/ERK kinase  ...[more]

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