Scripps VIVO scripps research logo

  • Index
  • Log in
  • Home
  • People
  • Organizations
  • Research
  • Events
Search form

Exploiting the polypharmacology of ß-carbolines to disrupt O. volvulus molting

Academic Article
uri icon
  • Overview
  • Research
  • Identity
  • Additional Document Info
  • View All
scroll to property group menus

Overview

authors

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

publication date

  • March 2015

journal

  • ACS Medicinal Chemistry Letters  Journal

abstract

  • Onchocerciasis is an infection caused by the filarial worm Onchocerca volvulus, which can eventually result in blindness. The lack of an effective macrofilaricide and the possible development of ivermectin-resistant strains of O. volvulus necessitate the need for alternative treatment strategies. We have shown that targeting the L3-stage-specific chitinase OvCHT1 impairs the shedding of the filarial cuticle. In our continued efforts to discover OvCHT1 inhibitors, we identified the β-carboline alkaloid scaffolding as a chitinase inhibitor that is capable of penetrating the worm cuticle. Herein, we disclose the rich polypharmacology of the β-carboline class of compounds as an approach to abrogate the molting of the parasite and thus the initiation of infection in the human host.
scroll to property group menus

Research

keywords

  • Onchocerciasis
  • beta-carbolines
  • chitinase inhibitor
  • polypharmacology
scroll to property group menus

Identity

PubMed Central ID

  • PMC4360149

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/ml500516r

PubMed ID

  • 25815157
scroll to property group menus

Additional Document Info

start page

  • 339

end page

  • 343

volume

  • 6

issue

  • 3

©2021 The Scripps Research Institute | Terms of Use | Powered by VIVO

  • About
  • Contact Us
  • Support