Literature DB >> 19362476

Low molecular weight non-peptide mimics of omega-conotoxin GVIA.

Peter J Duggan1, Richard J Lewis, Y Phei Lok, Natalie G Lumsden, Kellie L Tuck, Aijun Yang.   

Abstract

We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide omega-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193g/mol compared to a previously reported lead. This compound exhibits an EC(50) of 5.8microM and is accessible in only six synthetic steps compared to the original lead (13 steps). We also report several improvements to the original synthetic route.

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Year:  2009        PMID： 19362476     DOI： 10.1016/j.bmcl.2009.03.130

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

Review 1.  Targeting voltage-gated calcium channels: developments in peptide and small-molecule inhibitors for the treatment of neuropathic pain.

Authors:  S Vink; P F Alewood
Journal:  Br J Pharmacol       Date:  2012-11       Impact factor: 8.739

2.  Aminothiazolomorphinans with mixed κ and μ opioid activity.

Authors:  Tangzhi Zhang; Zhaohua Yan; Anna Sromek; Brian I Knapp; Thomas Scrimale; Jean M Bidlack; John L Neumeyer
Journal:  J Med Chem       Date:  2011-02-25       Impact factor: 7.446

3.  Inhibition of human N- and T-type calcium channels by an ortho-phenoxyanilide derivative, MONIRO-1.

Authors:  Jeffrey R McArthur; Leonid Motin; Ellen C Gleeson; Sandro Spiller; Richard J Lewis; Peter J Duggan; Kellie L Tuck; David J Adams
Journal:  Br J Pharmacol       Date:  2017-07-21       Impact factor: 8.739

4.  Antitumor and antimicrobial activity of some cyclic tetrapeptides and tripeptides derived from marine bacteria.

Authors:  Subrata Chakraborty; Dar-Fu Tai; Yi-Chun Lin; Tzyy-Wen Chiou
Journal:  Mar Drugs       Date:  2015-05-15       Impact factor: 5.118

5.  Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives.

Authors:  Ellen C Gleeson; Janease E Graham; Sandro Spiller; Irina Vetter; Richard J Lewis; Peter J Duggan; Kellie L Tuck
Journal:  Mar Drugs       Date:  2015-04-13       Impact factor: 5.118

6.  ω-Conotoxin GVIA mimetics that bind and inhibit neuronal Ca(v)2.2 ion channels.

Authors:  Charlotte Elisabet Tranberg; Aijun Yang; Irina Vetter; Jeffrey R McArthur; Jonathan B Baell; Richard J Lewis; Kellie L Tuck; Peter J Duggan
Journal:  Mar Drugs       Date:  2012-10-22       Impact factor: 6.085

Review 7.  Strategies for the development of conotoxins as new therapeutic leads.

Authors:  Ryan M Brady; Jonathan B Baell; Raymond S Norton
Journal:  Mar Drugs       Date:  2013-06-28       Impact factor: 5.118

Review 8.  Bioactive Mimetics of Conotoxins and other Venom Peptides.

Authors:  Peter J Duggan; Kellie L Tuck
Journal:  Toxins (Basel)       Date:  2015-10-16       Impact factor: 4.546
  8 in total

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