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

Belen Vaz; Sabine Möcklinghoff; Simon Folkertsma; Scott Lusher; Jacob de Vlieg; Luc Brunsveld

doi:10.1039/B910677D

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 Vlieg^b^c and Luc Brunsveld*^a^d

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.

Supplementary files

Publication details

The article was received on 01 Jun 2009, accepted on 20 Jul 2009 and first published on 17 Aug 2009

Article type: Communication

DOI: 10.1039/B910677D

Citation: Chem. Commun., 2009,0, 5377-5379

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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, 0, 5377
DOI: 10.1039/B910677D
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Chemical Communications

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

Abstract

Supplementary files

Publication details

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

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