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Synthesis and evaluation of oxyguanidine analogues of the cysteine protease inhibitor WRR-483 against cruzain

Academic Article
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Overview

authors

  • Jones, B. D.
  • Tochowicz, A.
  • Tang, Y.
  • Cameron, Michael
  • McCall, L. I.
  • Hirata, K.
  • Siqueira-Neto, J. L.
  • Reed, S. L.
  • McKerrow, J. H.
  • Roush, William

publication date

  • January 2016

journal

  • ACS Medicinal Chemistry Letters  Journal

abstract

  • A series of oxyguanidine analogues of the cysteine protease inhibitor WRR-483 were synthesized and evaluated against cruzain, the major cysteine protease of the protozoan parasite Trypanosoma cruzi. Kinetic analyses of these analogues indicated that they have comparable potency to previously prepared vinyl sulfone cruzain inhibitors. Co-crystal structures of the oxyguanidine analogues WRR-666 (4) and WRR-669 (7) bound to cruzain demonstrated different binding interactions with the cysteine protease, depending on the aryl moiety of the P1' inhibitor subunit. Specifically, these data demonstrate that WRR-669 is bound noncovalently in the crystal structure. This represents a rare example of noncovalent inhibition of a cysteine protease by a vinyl sulfone inhibitor.
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Research

keywords

  • Chagas' disease
  • X-ray crystallography
  • cysteine protease inhibitor
  • kinetics
  • noncovalent inhibitor
  • vinyl sulfone
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Identity

PubMed Central ID

  • PMC4716606

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/acsmedchemlett.5600336

PubMed ID

  • 26819670
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Additional Document Info

start page

  • 77

end page

  • 82

volume

  • 7

issue

  • 1

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