Cargando…

TRP channels as potential targets for antischistosomals

Ion channels are membrane protein complexes that underlie electrical excitability in cells, allowing ions to diffuse through cell membranes in a regulated fashion. They are essential for normal functioning of the neuromusculature and other tissues. Ion channels are also validated targets for many cu...

Descripción completa

Detalles Bibliográficos
Autores principales: Bais, Swarna, Greenberg, Robert M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6287577/
https://www.ncbi.nlm.nih.gov/pubmed/30224169
http://dx.doi.org/10.1016/j.ijpddr.2018.08.003
_version_ 1783379666728386560
author Bais, Swarna
Greenberg, Robert M.
author_facet Bais, Swarna
Greenberg, Robert M.
author_sort Bais, Swarna
collection PubMed
description Ion channels are membrane protein complexes that underlie electrical excitability in cells, allowing ions to diffuse through cell membranes in a regulated fashion. They are essential for normal functioning of the neuromusculature and other tissues. Ion channels are also validated targets for many current anthelmintics, yet the properties of only a small subset of ion channels in parasitic helminths have been explored in any detail. Transient receptor potential (TRP) channels comprise a widely diverse superfamily of ion channels with important roles in sensory signaling, regulation of ion homeostasis, organellar trafficking, and other functions. There are several subtypes of TRP channels, including TRPA1 and TRPV1 channels, both of which are involved in, among other functions, sensory, nociceptive, and inflammatory signaling in mammals. Several lines of evidence indicate that TRPA1-like channels in schistosomes exhibit pharmacological sensitivities that differ from their mammalian counterparts and that may signify unique physiological properties as well. Thus, in addition to responding to TRPA1 modulators, schistosome TRPA1-like channels also respond to compounds that in other organisms modulate TRPV1 channels. Notably, TRPV channel genes are not found in schistosome genomes. Here, we review the evidence leading to these conclusions and examine potential implications. We also discuss recent results showing that praziquantel, the current drug of choice against schistosomiasis, selectively targets host TRP channels in addition to its likely primary targets in the parasite. The results we discuss add weight to the notion that schistosome TRP channels are worthy of investigation as candidate therapeutic targets.
format Online
Article
Text
id pubmed-6287577
institution National Center for Biotechnology Information
language English
publishDate 2018
publisher Elsevier
record_format MEDLINE/PubMed
spelling pubmed-62875772018-12-19 TRP channels as potential targets for antischistosomals Bais, Swarna Greenberg, Robert M. Int J Parasitol Drugs Drug Resist Articles from the scientific meeting: "Anthelmintics: From Discovery to Resistance III", pp. 494 - 628. Ion channels are membrane protein complexes that underlie electrical excitability in cells, allowing ions to diffuse through cell membranes in a regulated fashion. They are essential for normal functioning of the neuromusculature and other tissues. Ion channels are also validated targets for many current anthelmintics, yet the properties of only a small subset of ion channels in parasitic helminths have been explored in any detail. Transient receptor potential (TRP) channels comprise a widely diverse superfamily of ion channels with important roles in sensory signaling, regulation of ion homeostasis, organellar trafficking, and other functions. There are several subtypes of TRP channels, including TRPA1 and TRPV1 channels, both of which are involved in, among other functions, sensory, nociceptive, and inflammatory signaling in mammals. Several lines of evidence indicate that TRPA1-like channels in schistosomes exhibit pharmacological sensitivities that differ from their mammalian counterparts and that may signify unique physiological properties as well. Thus, in addition to responding to TRPA1 modulators, schistosome TRPA1-like channels also respond to compounds that in other organisms modulate TRPV1 channels. Notably, TRPV channel genes are not found in schistosome genomes. Here, we review the evidence leading to these conclusions and examine potential implications. We also discuss recent results showing that praziquantel, the current drug of choice against schistosomiasis, selectively targets host TRP channels in addition to its likely primary targets in the parasite. The results we discuss add weight to the notion that schistosome TRP channels are worthy of investigation as candidate therapeutic targets. Elsevier 2018-09-08 /pmc/articles/PMC6287577/ /pubmed/30224169 http://dx.doi.org/10.1016/j.ijpddr.2018.08.003 Text en © 2018 The Authors http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Articles from the scientific meeting: "Anthelmintics: From Discovery to Resistance III", pp. 494 - 628.
Bais, Swarna
Greenberg, Robert M.
TRP channels as potential targets for antischistosomals
title TRP channels as potential targets for antischistosomals
title_full TRP channels as potential targets for antischistosomals
title_fullStr TRP channels as potential targets for antischistosomals
title_full_unstemmed TRP channels as potential targets for antischistosomals
title_short TRP channels as potential targets for antischistosomals
title_sort trp channels as potential targets for antischistosomals
topic Articles from the scientific meeting: "Anthelmintics: From Discovery to Resistance III", pp. 494 - 628.
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6287577/
https://www.ncbi.nlm.nih.gov/pubmed/30224169
http://dx.doi.org/10.1016/j.ijpddr.2018.08.003
work_keys_str_mv AT baisswarna trpchannelsaspotentialtargetsforantischistosomals
AT greenbergrobertm trpchannelsaspotentialtargetsforantischistosomals