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Design and synthesis of dipeptidyl alpha',beta '-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain

Academic Article
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Overview

authors

  • Roush, William
  • Gonzalez, F. V.
  • McKerrow, J. H.
  • Hansell, E.

publication date

  • October 1998

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • The dipeptidyl epoxy ketone 4 is a potent, irreversible inhibitor of cruzain, a cysteine protease isolated from Trypanosoma cruzi, with an apparent second order inhibition rate constant of 330,000 sec-1M-1.

subject areas

  • Cysteine Endopeptidases
  • Cysteine Proteinase Inhibitors
  • Dipeptides
  • Drug Design
  • Ketones
  • Kinetics
  • Protozoan Proteins
  • Stereoisomerism
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(98)00494-6

PubMed ID

  • 9873627
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Additional Document Info

start page

  • 2809

end page

  • 2812

volume

  • 8

issue

  • 19

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