Issue 2, 2016
From the journal:

Organic & Biomolecular Chemistry

Targeting anti-apoptotic Bcl2 proteins with scyllatoxin-based BH3 domain mimetics†

M. Margaret Harris,a   Zachary Coon,a   Najah Alqaeisoom,a   Brian Swordsa  and  Justin M. Holub*a  

* Corresponding authors

a Department of Chemistry and Biochemistry, Ohio University, Athens, OH 45701, USA
E-mail: holub@ohio.edu
Fax: +1 740-597-1772
Tel: +1 740-597-1228

Abstract

BH3 domain mimetics based on the small protein scyllatoxin (ScTx) were designed to target the anti-apoptotic protein Bcl2 in vitro. Intrinsically disordered ScTx variants were found to bind Bcl2 with nanomolar affinity, indicating that an induced fit binding mechanism is required for favorable BH3 : Bcl2 interaction.

Graphical abstract: Targeting anti-apoptotic Bcl2 proteins with scyllatoxin-based BH3 domain mimetics

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Article information

DOI
https://doi.org/10.1039/C5OB02080H
Article type
Communication
Submitted
08 Oct 2015
Accepted
05 Nov 2015
First published
05 Nov 2015

Org. Biomol. Chem., 2016,14, 440-446

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Targeting anti-apoptotic Bcl2 proteins with scyllatoxin-based BH3 domain mimetics

M. M. Harris, Z. Coon, N. Alqaeisoom, B. Swords and J. M. Holub, Org. Biomol. Chem., 2016, 14, 440 DOI: 10.1039/C5OB02080H

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