Strategies for the Development of Conotoxins as New Therapeutic Leads

Peptide toxins typically bind to their target ion channels or receptors with high potency and selectivity, making them attractive leads for therapeutic development. In some cases the native peptide as it is found in the venom from which it originates can be used directly, but in many instances it is...

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Main Authors: Jonathan B. Baell, Ryan M. Brady, Raymond S. Norton
Format: Article
Language:English
Published: MDPI AG 2013-06-01
Series:Marine Drugs
Subjects:
Online Access:http://www.mdpi.com/1660-3397/11/7/2293
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spelling doaj-649b36f659cf4c7e9eaca10aa37cbfc82020-11-24T22:38:54ZengMDPI AGMarine Drugs1660-33972013-06-011172293231310.3390/md11072293Strategies for the Development of Conotoxins as New Therapeutic LeadsJonathan B. BaellRyan M. BradyRaymond S. NortonPeptide toxins typically bind to their target ion channels or receptors with high potency and selectivity, making them attractive leads for therapeutic development. In some cases the native peptide as it is found in the venom from which it originates can be used directly, but in many instances it is desirable to truncate and/or stabilize the peptide to improve its therapeutic properties. A complementary strategy is to display the key residues that make up the pharmacophore of the peptide toxin on a non-peptidic scaffold, thereby creating a peptidomimetic. This review exemplifies these approaches with peptide toxins from marine organisms, with a particular focus on conotoxins.http://www.mdpi.com/1660-3397/11/7/2293peptide toxinpeptidomimeticion channelpaincone snail
collection DOAJ
language English
format Article
sources DOAJ
author Jonathan B. Baell
Ryan M. Brady
Raymond S. Norton
spellingShingle Jonathan B. Baell
Ryan M. Brady
Raymond S. Norton
Strategies for the Development of Conotoxins as New Therapeutic Leads
Marine Drugs
peptide toxin
peptidomimetic
ion channel
pain
cone snail
author_facet Jonathan B. Baell
Ryan M. Brady
Raymond S. Norton
author_sort Jonathan B. Baell
title Strategies for the Development of Conotoxins as New Therapeutic Leads
title_short Strategies for the Development of Conotoxins as New Therapeutic Leads
title_full Strategies for the Development of Conotoxins as New Therapeutic Leads
title_fullStr Strategies for the Development of Conotoxins as New Therapeutic Leads
title_full_unstemmed Strategies for the Development of Conotoxins as New Therapeutic Leads
title_sort strategies for the development of conotoxins as new therapeutic leads
publisher MDPI AG
series Marine Drugs
issn 1660-3397
publishDate 2013-06-01
description Peptide toxins typically bind to their target ion channels or receptors with high potency and selectivity, making them attractive leads for therapeutic development. In some cases the native peptide as it is found in the venom from which it originates can be used directly, but in many instances it is desirable to truncate and/or stabilize the peptide to improve its therapeutic properties. A complementary strategy is to display the key residues that make up the pharmacophore of the peptide toxin on a non-peptidic scaffold, thereby creating a peptidomimetic. This review exemplifies these approaches with peptide toxins from marine organisms, with a particular focus on conotoxins.
topic peptide toxin
peptidomimetic
ion channel
pain
cone snail
url http://www.mdpi.com/1660-3397/11/7/2293
work_keys_str_mv AT jonathanbbaell strategiesforthedevelopmentofconotoxinsasnewtherapeuticleads
AT ryanmbrady strategiesforthedevelopmentofconotoxinsasnewtherapeuticleads
AT raymondsnorton strategiesforthedevelopmentofconotoxinsasnewtherapeuticleads
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