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Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

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.

Thomas Bohnacker
Andrea E. Prota
Matthias P. Wymann
ResearchOpen Access09 Mar 2017
Nature Communications

Volume: 8, P: 1-13
Dimethyl fumarate in patients admitted to hospital with COVID-19 (RECOVERY): a randomised, controlled, open-label, platform trial

Dimethyl fumarate (DMF) is an anti-inflammatory drug proposed as a treatment for COVID19. Here the results are reported from a randomised trial testing DMF treatment in 713 patients hospitalised with COVID-19. DMF was not associated with any improvement in day 5 outcomes.

Peter Sandercock
Janet Darbyshire
Martin J. Landray
ResearchOpen Access31 Jan 2024
Nature Communications

Volume: 15, P: 1-13
A class of highly selective inhibitors bind to an active state of PI3Kγ

Combining X-ray structures, surface plasmon resonance and hydrogen-deuterium exchange–mass spectrometry, a class of highly selective inhibitors was found to bind to an active state of PI3Kγ breaking a conformational ‘lock’ important for activation of PI3Kγ.

Gangadhara Gangadhara
Göran Dahl
Jens Petersen
Research04 Feb 2019
Nature Chemical Biology

Volume: 15, P: 348-357

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Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

Dimethyl fumarate in patients admitted to hospital with COVID-19 (RECOVERY): a randomised, controlled, open-label, platform trial

A class of highly selective inhibitors bind to an active state of PI3Kγ

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