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Issue 36, 2009
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Computational design, synthesis, and evaluation of miniproteins as androgen receptor coactivator mimics†

Belen Vaz,a   Sabine Möcklinghoff,a   Simon Folkertsma,b   Scott Lusher,c   Jacob de Vliegbc  and  Luc Brunsveld*ad  
Author affiliations

* Corresponding authors

a Chemical Genomics Centre of the Max Planck Society, Otto-Hahn Straße 15, 44227 Dortmund, Germany

b Computational Drug Discovery, Centre for Molecular and Biomolecular Informatics, Radboud University, Nijmegen, The Netherlands

c Molecular Design & Informatics, Schering-Plough, Oss, The Netherlands

d Laboratory of Chemical Biology, Department of Biomedical Engineering, Technische Universiteit Eindhoven, Den Dolech 2, Eindhoven, The Netherlands
E-mail: l.brunsveld@tue.nl
Fax: +31 402478367

Abstract

Insertion of 3 to 4 mutations, based on in silico modelling, in a diverse set of natural miniproteins generates potent androgen receptor (AR) binders and a clear insight into the structure–activity relationship of such coactivator mimics concerning helix length.

Graphical abstract: Computational design, synthesis, and evaluation of miniproteins as androgen receptor coactivator mimics

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Article information

https://doi.org/10.1039/B910677D
Submitted
01 Jun 2009
Accepted
20 Jul 2009
First published
17 Aug 2009
Chem. Commun., 2009, 5377-5379
Article type
Communication
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Computational design, synthesis, and evaluation of miniproteins as androgen receptor coactivator mimics

B. Vaz, S. Möcklinghoff, S. Folkertsma, S. Lusher, J. de Vlieg and L. Brunsveld, Chem. Commun., 2009, 5377
DOI: 10.1039/B910677D

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