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BIBTEX RIS

Discovery of Macrocyclic Peptides Armed with a Mechanism‐Based Warhead: Isoform‐Selective Inhibition of Human Deacetylase SIRT2

2012; Wiley; Volume: 51; Issue: 14 Linguagem: Inglês

10.1002/anie.201108118

ISSN

1521-3773

Autores

Jumpei Morimoto, Yuuki Hayashi, Hiroaki Suga,

Tópico(s)

Sirtuins and Resveratrol in Medicine

Resumo

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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