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. 2012 Apr 2;51(14):3423-7.
doi: 10.1002/anie.201108118. Epub 2012 Feb 28.

Discovery of macrocyclic peptides armed with a mechanism-based warhead: isoform-selective inhibition of human deacetylase SIRT2

Jumpei Morimoto  1 , Yuuki Hayashi, Hiroaki Suga
Affiliations

Discovery of macrocyclic peptides armed with a mechanism-based warhead: isoform-selective inhibition of human deacetylase SIRT2

Jumpei Morimoto et al. Angew Chem Int Ed Engl. .

Abstract

Designed to inhibit: by using the random nonstandard peptide integrated discovery (RaPID) system, highly potent isoform-selective inhibitors can be identified from a library of nonstandard macrocyclic peptides. These inhibitors, which contain a mechanism-based warhead residue, are active against the human deacetylase SIRT2, with IC(50) values in the low nanomolar region.

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