학술논문
Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
Document Type
article
Author
Thomas Bohnacker; Andrea E. Prota; Florent Beaufils; John E. Burke; Anna Melone; Alison J. Inglis; Denise Rageot; Alexander M. Sele; Vladimir Cmiljanovic; Natasa Cmiljanovic; Katja Bargsten; Amol Aher; Anna Akhmanova; J. Fernando Díaz; Doriano Fabbro; Marketa Zvelebil; Roger L. Williams; Michel O. Steinmetz; Matthias P. Wymann
Source
Nature Communications, Vol 8, Iss 1, Pp 1-13 (2017)
Subject
Language
English
ISSN
2041-1723
Abstract
Buparlisib/BKM120 is in phase 3 clinical trials as a phosphoinositide 3-kinase (PI3K) inhibitor. Here, Bohnackeret al. combine chemical biology and structural biology approaches to segregate BKM120’s biological actions, and suggest that it causes mitotic arrest predominantly by binding microtubules and disrupting their dynamics.