Strategies for the Development of Conotoxins as New Therapeutic Leads

Marine Drugs

Ryan M. Brady¹  Jonathan B. Baell¹ 

[1] Monash Institute of Pharmaceutical Science, Monash University, 381 Royal Parade, Parkville 3052, Australia;

关键词: peptide toxin;    peptidomimetic;    ion channel;    pain;    cone snail;   

DOI  :  10.3390/md11072293

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.