Selective Inhibition of BFL1: It's All about Finding the Right Partner

Haiming Dai; X. Wei Meng; Scott H. Kaufmann

doi:10.1016/j.chembiol.2020.05.014

Selective Inhibition of BFL1: It's All about Finding the Right Partner

Haiming Dai, X. Wei Meng, Scott H. Kaufmann

Oncology

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

Abstract

In this issue of Cell Chemical Biology, Harvey et al. (2020) identify 4E14, a sulfhydryl-containing N-acetyltryptophan analog that selectively disrupts binding to the previously undruggable anti-apoptotic BCL2 paralog BFL1, and elucidate a BFL1 conformational change that facilitates 4E14 interaction. These results provide insight that will accelerate development of BFL1 inhibitors.

Original language	English (US)
Pages (from-to)	639-642
Number of pages	4
Journal	Cell Chemical Biology
Volume	27
Issue number	6
DOIs	https://doi.org/10.1016/j.chembiol.2020.05.014
State	Published - Jun 18 2020

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmacology
Drug Discovery
Clinical Biochemistry

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10.1016/j.chembiol.2020.05.014

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title = "Selective Inhibition of BFL1: It's All about Finding the Right Partner",

abstract = "In this issue of Cell Chemical Biology, Harvey et al. (2020) identify 4E14, a sulfhydryl-containing N-acetyltryptophan analog that selectively disrupts binding to the previously undruggable anti-apoptotic BCL2 paralog BFL1, and elucidate a BFL1 conformational change that facilitates 4E14 interaction. These results provide insight that will accelerate development of BFL1 inhibitors.",

author = "Haiming Dai and Meng, {X. Wei} and Kaufmann, {Scott H.}",

note = "Funding Information: We gratefully acknowledge research support from the NCI ( R01 CA166741 and R01 CA172503 ) as well as assistance from Kaiqin Ye in preparing Figure 1 C. Publisher Copyright: {\textcopyright} 2020 Elsevier Ltd",

year = "2020",

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doi = "10.1016/j.chembiol.2020.05.014",

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AU - Dai, Haiming

AU - Meng, X. Wei

AU - Kaufmann, Scott H.

N1 - Funding Information: We gratefully acknowledge research support from the NCI ( R01 CA166741 and R01 CA172503 ) as well as assistance from Kaiqin Ye in preparing Figure 1 C. Publisher Copyright: © 2020 Elsevier Ltd

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Y1 - 2020/6/18

N2 - In this issue of Cell Chemical Biology, Harvey et al. (2020) identify 4E14, a sulfhydryl-containing N-acetyltryptophan analog that selectively disrupts binding to the previously undruggable anti-apoptotic BCL2 paralog BFL1, and elucidate a BFL1 conformational change that facilitates 4E14 interaction. These results provide insight that will accelerate development of BFL1 inhibitors.

AB - In this issue of Cell Chemical Biology, Harvey et al. (2020) identify 4E14, a sulfhydryl-containing N-acetyltryptophan analog that selectively disrupts binding to the previously undruggable anti-apoptotic BCL2 paralog BFL1, and elucidate a BFL1 conformational change that facilitates 4E14 interaction. These results provide insight that will accelerate development of BFL1 inhibitors.

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Selective Inhibition of BFL1: It's All about Finding the Right Partner

Abstract

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