ω-conotoxins gvia, mviia and cvid sar and clinical potentialω-conotoxins gvia mviia cvid sar和临床潜力.pdfVIP
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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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