Allosteric sensitization of proapoptotic BAX

Jonathan R. Pritz,Franziska Wachter,Susan Lee,James Luccarelli,Thomas E. Wales,Daniel Cohen,Paul Coote,Gregory J. Heffron,John R. Engen,Walter Massefski,Loren D. Walensky

Allosteric sensitization of proapoptotic BAX

2017

Jonathan R. Pritz
Franziska Wachter
Susan Lee
James Luccarelli
Thomas E. Wales
Daniel Cohen
Paul Coote
Gregory J. Heffron
John R. Engen
Walter Massefski
Loren D. Walensky

An NMR fragment screen identified a small molecule that binds to an allosteric site on the proapoptotic protein BAX and synergizes with the BIM BH3 domain to conformationally activate BAX and enhance BAX-mediated membrane poration.

Keywords:

Molecular biology
Nuclear magnetic resonance spectroscopy
Small molecule
Biochemistry
Programmed cell death
Biology
Sensitization
Membrane protein
Membrane
Cell biology
Allosteric regulation
Chemistry
Bcl-2 family
Apoptosis

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