Conotoxins: Structure, Therapeutic Potential and Pharmacological Applications

Abstract

Cone snails, also known as marine gastropods, from Conus genus produce in their venom a diverse range of small pharmacologically active structured peptides called conotoxins. The cone snail venoms are widely unexplored arsenal of toxins with therapeutic and pharmacological potential, making them a treasure trove of ligands and peptidic drug leads. Conotoxins are small disulphide bonded peptides which act as remarkable selective inhibitors and modulators of ion channels (calcium, sodium, potassium), nicotinic acetylcholine receptors, noradrenaline transporters, N-methyl-D-aspartate receptors, and neurotensin receptors. They are highly potent and specific against several neuronal targets making them valuable as research tools, drug leads and even therapeutics. In this review we discuss their gene superfamily classification, nomenclature, post-translational modification, structural framework, pharmacology and medical applications of the active conopeptides. We aim to give an overview of their structure and therapeutic potential. Understanding these aspects of conopeptides will help in designing more specific peptidic analogues.

Relative Citation Ratio (RCR): A New Metric That Uses Citation Rates to Measure Influence at the Article Level

“…By leveraging this expertise, networks define empirical field boundaries that are simultaneously more flexible and more precise than those imposed by traditional bibliometric categories such as “biology and biochemistry” or “molecular biology.” An analysis of the co-citation network of a sample RA illustrates this point. The RA in the bottom panel of Fig 1B describes the identification of new peptides structurally similar to conotoxins, a little-known family of proteins that has begun to attract attention as the result of recent work describing their potential clinical utility [36]. Although the papers in this network are all highly relevant to the study of conotoxins, they cross traditional disciplinary boundaries to include such diverse fields as evolutionary biology, structural biology, biochemistry, genetics, and pharmacology (Fig 1C).…”

Residues Responsible for the Selectivity of α-Conotoxins for Ac-AChBP or nAChRs

“…α-Conotoxins, which come from sea Conus snails, are important tool for studying nAChRs. They are also used as pharmacological probes and as potential therapeutic agents for the treatment of severe pain [6,7,8,9,10,11,12]. α-Conotoxins are diverse and target a variety of nAChR subtypes.…”

Peptides, Peptidomimetics, and Polypeptides from Marine Sources: A Wealth of Natural Sources for Pharmaceutical Applications

“…Such structures can be used as templates for designing rapid-acting therapeutic insulin for diabetic patients. Characterizations of conotoxins and their pharmaceutical applications have also been described in review articles [54,148,149]. …”