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Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting

Academic Article
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Overview

authors

  • Gooyit, M.
  • Tricoche, N.
  • Lustigman, S.
  • Janda, Kim

publication date

  • July 2014

journal

  • Journal of Medicinal Chemistry  Journal

abstract

  • The L3-stage-specific chitinase OvCHT1 has been implicated in the development of Onchocerca volvulus, the causative agent of onchocerciasis. Closantel, a known anthelmintic drug, was previously discovered as a potent and specific OvCHT1 inhibitor. As closantel is also a known protonophore, we performed a simple scaffold modulation to map out the structural features that are relevant for its individual or dual biochemical roles. Furthermore, we present that either OvCHT1 inhibition or protonophoric activity was capable of affecting O. volvulus L3 molting and that the presence of both activities in a single molecule yielded more potent inhibition of the nematode's developmental process.

subject areas

  • Animals
  • Antinematodal Agents
  • Caenorhabditis elegans
  • Chitinase
  • Enzyme Inhibitors
  • Ionophores
  • Molting
  • Onchocerca volvulus
  • Onchocerciasis
  • Salicylanilides
  • Structure-Activity Relationship
  • Uncoupling Agents
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Identity

PubMed Central ID

  • PMC4216208

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm5006435

PubMed ID

  • 24918716
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Additional Document Info

start page

  • 5792

end page

  • 5799

volume

  • 57

issue

  • 13

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