Issue 75, 2012
From the journal:

Chemical Communications

Application of an omonasteine ligation strategy for the total chemical synthesis of the BRD7 bromodomain†

Pieter Van de Vijver,*a   Liesbeth Scheer,a   Judy van Beijnum,b   Arjan Griffioenb  and  Tilman M. Hackeng*a  

* Corresponding authors

a Laboratory for Chemical Protein Synthesis, Department of Biochemistry, Maastricht University, Universiteitssingel 50, Maastricht, The Netherlands
E-mail: p.vandevijver@maastrichtuniversity.nl, t.hackeng@maastrichtuniversity.nl
Fax: +31 43 388 4159
Tel: +31 43 388 1674

b Angiogenesis Laboratory, Department of Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands

Abstract

The use of omonasteine (Omo) in sequential peptide ligation strategies extends the scope of homocysteine (Hcy) ligation to longer, methionine-rich proteins. Hcy-to-Omo conversion can be performed on-resin, while the Omo-to-Hcy deprotection can be performed in situ after peptide ligation. This strategy was successfully applied in the synthesis of the BRD7 bromodomain.

Graphical abstract: Application of an omonasteine ligation strategy for the total chemical synthesis of the BRD7 bromodomain

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Article information

DOI
https://doi.org/10.1039/C2CC34956F
Article type
Communication
Submitted
11 Jul 2012
Accepted
25 Jul 2012
First published
30 Jul 2012

Chem. Commun., 2012,48, 9403-9405

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Application of an omonasteine ligation strategy for the total chemical synthesis of the BRD7 bromodomain

P. Van de Vijver, L. Scheer, J. van Beijnum, A. Griffioen and T. M. Hackeng, Chem. Commun., 2012, 48, 9403 DOI: 10.1039/C2CC34956F

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