B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins

Thibaud T. Renault; Rana Elkholi; Archana Bharti; Jerry E. Chipuk

doi:10.1074/jbc.M114.569632

B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins

Thibaud T. Renault
, Rana Elkholi
, Archana Bharti
, Jerry E. Chipuk

Research output: Contribution to journal › Article › peer-review

31 Scopus citations

Abstract

Background: BH3 mimetics are promising chemotherapeutics, but their full mechanisms of action are underexplored.

Results: BAX, BID, and BIM directly influence BH3 mimetics to pharmacologically inhibit anti-apoptotic BCL-2 proteins.

Conclusion: BH3 mimetics display differential activities that are dependent upon both anti- and proapoptotic BCL-2 members function.

Significance: Understanding how BH3 mimetics function within the BCL-2 family repertoire will improve the utility of these drugs.

Original language	English
Pages (from-to)	26481-26491
Number of pages	11
Journal	Journal of Biological Chemistry
Volume	289
Issue number	38
DOIs	https://doi.org/10.1074/jbc.M114.569632
State	Published - 19 Sep 2014

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title = "B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins",

abstract = "Background: BH3 mimetics are promising chemotherapeutics, but their full mechanisms of action are underexplored.Results: BAX, BID, and BIM directly influence BH3 mimetics to pharmacologically inhibit anti-apoptotic BCL-2 proteins.Conclusion: BH3 mimetics display differential activities that are dependent upon both anti- and proapoptotic BCL-2 members function.Significance: Understanding how BH3 mimetics function within the BCL-2 family repertoire will improve the utility of these drugs.",

author = "Renault, \{Thibaud T.\} and Rana Elkholi and Archana Bharti and Chipuk, \{Jerry E.\}",

note = "Publisher Copyright: {\textcopyright} 2014 by The American Society for Biochemistry and Molecular Biology, Inc.",

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B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins. / Renault, Thibaud T.; Elkholi, Rana; Bharti, Archana et al.
In: Journal of Biological Chemistry, Vol. 289, No. 38, 19.09.2014, p. 26481-26491.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins

AU - Renault, Thibaud T.

AU - Elkholi, Rana

AU - Bharti, Archana

AU - Chipuk, Jerry E.

PY - 2014/9/19

Y1 - 2014/9/19

N2 - Background: BH3 mimetics are promising chemotherapeutics, but their full mechanisms of action are underexplored.Results: BAX, BID, and BIM directly influence BH3 mimetics to pharmacologically inhibit anti-apoptotic BCL-2 proteins.Conclusion: BH3 mimetics display differential activities that are dependent upon both anti- and proapoptotic BCL-2 members function.Significance: Understanding how BH3 mimetics function within the BCL-2 family repertoire will improve the utility of these drugs.

AB - Background: BH3 mimetics are promising chemotherapeutics, but their full mechanisms of action are underexplored.Results: BAX, BID, and BIM directly influence BH3 mimetics to pharmacologically inhibit anti-apoptotic BCL-2 proteins.Conclusion: BH3 mimetics display differential activities that are dependent upon both anti- and proapoptotic BCL-2 members function.Significance: Understanding how BH3 mimetics function within the BCL-2 family repertoire will improve the utility of these drugs.

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B cell lymphoma-2 (BCL-2) homology domain 3 (BH3) mimetics demonstrate differential activities dependent upon the functional repertoire of pro- and anti-apoptotic BCL-2 family proteins

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