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Epistatic mutations in PUMA BH3 drive an alternate binding mode to potently and selectively inhibit anti-apoptotic Bfl-1

Overexpression of anti-apoptotic Bcl-2 family proteins contributes to cancer progression and confers resistance to chemotherapy. Small molecules that target Bcl-2 are used in the clinic to treat leukemia, but tight and selective inhibitors are not available for Bcl-2 paralog Bfl-1. Guided by computa...

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Detalles Bibliográficos
Autores principales: Jenson, Justin M, Ryan, Jeremy A, Grant, Robert A, Letai, Anthony, Keating, Amy E
Formato: Online Artículo Texto
Lenguaje:English
Publicado: eLife Sciences Publications, Ltd 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5464773/
https://www.ncbi.nlm.nih.gov/pubmed/28594323
http://dx.doi.org/10.7554/eLife.25541