mu-Conotoxins as Leads in the Development of New Analgesics
- Author(s)
- Norton, RS;
- Details
- Publication Year 2010-04,Volume 15,Issue #4,Page 2825-2844
- Journal Title
- MOLECULES
- Publication Type
- Journal Article
- Abstract
- Voltage-gated sodium channels (VGSCs) contain a specific binding site for a family of cone shell toxins known as mu-conotoxins. As some VGSCs are involved in pain perception and mu-conotoxins are able to block these channels, mu-conotoxins show considerable potential as analgesics. Recent studies have advanced our understanding of the three-dimensional structures and structure-function relationships of the mu-conotoxins, including their interaction with VGSCs. Truncated peptide analogues of the native toxins have been created in which secondary structure elements are stabilized by non-native linkers such as lactam bridges. Ultimately, it would be desirable to capture the favourable analgesic properties of the native toxins, in particular their potency and channel sub-type selectivity, in non-peptide mimetics. Such mimetics would constitute lead compounds in the development of new therapeutics for the treatment of pain.
- Publisher
- MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI
- Keywords
- RESISTANT SODIUM-CHANNELS; SPINAL SENSORY NEURONS; DORSAL-ROOT GANGLIA; ALPHA-HELIX MIMICRY; SHK TOXIN; CHEMICAL-SYNTHESIS; CONUS-STRIATUS; BINDING-SITE; SIDE-CHAIN; BIOLOGICAL EVALUATION
- Publisher's Version
- https://doi.org/10.3390/molecules15042825
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2010-04-01 12:00:00