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Probing the bioactive conformation of an archetypal natural product HDAC inhibitor with conformationally homogeneous triazole-modified cyclic tetrapeptides

Academic Article
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Overview

related to degree

  • Beierle, John Michael, Ph.D. in Chemistry, Scripps Research 2004 - 2009
  • Horne, William Seth, Ph.D. in Chemistry, Scripps Research 2000 - 2005

authors

  • Horne, William Seth
  • Olsen, C. A.
  • Beierle, John Michael
  • Montero, A.
  • Ghadiri, M. Reza

publication date

  • 2009

journal

  • Angewandte Chemie-International Edition  Journal

abstract

  • Fooling enzymes with mock amides: Analogues of apicidin, a cyclic-tetrapeptide inhibitor of histone deacetylase (HDAC), were designed with a 1,4- or 1,5-disubstituted 1,2,3-triazole in place of a backbone amide bond to fix the bond in question in either a trans-like or a cis-like configuration. Thus, the binding affinity of distinct peptide conformations (see picture) could be probed. One analogue proved in some cases to be superior to apicidin as an HDAC inhibitor.

subject areas

  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Histone Deacetylases
  • Peptides, Cyclic
  • Protein Conformation
  • Stereoisomerism
  • Structure-Activity Relationship
  • Triazoles
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Research

keywords

  • cyclic peptides
  • drug design
  • enzyme inhibitors
  • structure-activity relationships
  • triazoles
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Identity

PubMed Central ID

  • PMC3041267

International Standard Serial Number (ISSN)

  • 1433-7851

Digital Object Identifier (DOI)

  • 10.1002/anie.200805900

PubMed ID

  • 19267380
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Additional Document Info

start page

  • 4718

end page

  • 4724

volume

  • 48

issue

  • 26

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