mu-Conotoxins as Leads in the Development of New Analgesics

作者：Norton Raymond S^*

来源：Molecules, 2010, 15(4): 2825-2844.

DOI：10.3390/molecules15042825

• cone shell
• toxin
• sodium channel
• pain
• peptide mimetic

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.

• 出版日期2010-4
• 单位河北医科大学