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ω-conotoxins gvia, mviia and cvid sar and clinical potentialω-conotoxins gvia mviia cvid sar和临床潜力
Mar. Drugs 2006, 4, 193-214 Marine Drugs ISSN 1660-3397 © 2006 by MDPI /marinedrugs Special Issue on “Marine Drugs and Ion Channels” Edited by Hugo Arias Review ω-Conotoxins GVIA, MVIIA and CVID: SAR and Clinical Potential Christina I. Schroeder and Richard J. Lewis* Institute for Molecular Bioscience, The University of Queensland, St Lucia, 4072, QLD, Australia E-mail: t.schroeder@.au (for Christina I. Schroeder) * To whom correspondence should be addressed. Tel: +61-7-3346 2984; Fax: +61-7-3346 2101. E-mail: r.lewis@.au Received: 16 February 2006 / Accepted: 28 February 2006 / Published: 6 April 2006 Abstract: Highly selective N-type voltage-gated calcium (Ca ) channel inhibitors from V cone snail venom (the ω-conotoxins) have emerged as a new class of therapeutics for the treatment of chronic and neuropathic pain. Earlier in 2005, Prialt (Elan) or synthetic ω- conotoxin MVIIA, was the first ω-conotoxin to be approved by Food and Drug Administration for human use. This review compares the action of three ω-conotoxins, GVIA, MVIIA and CVID, describing their structure-activity relationships and potential as leads for the design of improved N-type therapeutics that are more useful in the treatment of chronic pain. Keywords: ω-conotoxin, Structure-Activity relationship, pain. Abbreviations: FDA, Food and Drug Administration; AChR, nicotinic ac
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