Issue 32, 2015
From the journal:

Organic & Biomolecular Chemistry

Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold†

M. E. Lanning,a   P. T. Wilder,bc   H. Bailey,d   B. Drennen,a   M. Cavalier,bc   L. Chen,a   J. L. Yap,a   M. Rajea  and  S. Fletcher*ac  

* Corresponding authors

a Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N. Pine St., Baltimore, MD 21201, USA
E-mail: sfletcher@rx.umaryland.edu

b Department of Biochemistry, University of Maryland School of Medicine, 22 S. Greene St., Baltimore, MD 21201, USA

c University of Maryland Greenebaum Cancer Center, 22 S. Greene St., Baltimore, MD 21201, USA

d Bryn Mawr School, 109 W. Melrose Ave., Baltimore, MD 21210, USA

Abstract

Mimicry of two faces of an α-helix might yield more potent and more selective inhibitors of aberrant, helix-mediated protein–protein interactions (PPI). Herein, we demonstrate that a 2,6,9-tri-substituted purine is capable of disrupting the Mcl-1-Bak-BH3 PPI through effective mimicry of key residues on opposing faces of the Bak-BH3 α-helix.

Graphical abstract: Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold

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Article information

DOI
https://doi.org/10.1039/C5OB00478K
Article type
Communication
Submitted
11 Mar 2015
Accepted
09 Jul 2015
First published
09 Jul 2015

Org. Biomol. Chem., 2015,13, 8642-8646

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Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold

M. E. Lanning, P. T. Wilder, H. Bailey, B. Drennen, M. Cavalier, L. Chen, J. L. Yap, M. Raje and S. Fletcher, Org. Biomol. Chem., 2015, 13, 8642 DOI: 10.1039/C5OB00478K

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