BH3-Only Mimetics

Living reference work entry

Abstract

BH3 mimetics are a class of drugs designed to tip the balance of pro- and anti-apoptotic factors within a cell to favor apoptosis. They bind within a specific groove of anti-apoptotic Bcl-2 family survival factors in a similar manner to native proteins within the cell that regulate these factors. This primes the cell for apoptosis. Several small molecule BH3 mimetics are currently undergoing evaluation in clinical trials.

Keywords

ABT-737 Anti-apoptotic Bcl-2 family Bad Bcl-2 ABT-737 and ABT-263 Assessment B-cell lymphoma and mantle cell lymphoma BH3-only mimetics BH3-only proteins Clinical trials CLL and ALL Gossypol Hydrocarbon stapling Mcl-1 overexpression Navitoclax Obatoclax Preclinical studies Role in cancer BH3-only proteins Activators Chemotherapy Overall survival in glioblastoma multiforme Predictors of survival Sensitizers Therapeutics Bid Bim Pro-apoptotic Bcl-2 proteins Puma and Noxa 

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Copyright information

© Springer Science Business Media, New York (outside the USA) 2014

Authors and Affiliations

  1. 1.National Institutes of Health, Center for Cancer Research, National Cancer InstituteBethesdaUSA

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