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Low molecular weight non-peptide mimics of omega-conotoxin GVIA.
Duggan, Peter J; Lewis, Richard J; Phei Lok, Y; Lumsden, Natalie G; Tuck, Kellie L; Yang, Aijun.
Affiliation
  • Duggan PJ; CSIRO Molecular and Health Technologies, Clayton, VIC, Australia.
Bioorg Med Chem Lett ; 19(10): 2763-5, 2009 May 15.
Article in En | MEDLINE | ID: mdl-19362476
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Calcium Channel Blockers / Omega-Conotoxin GVIA Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Calcium Channel Blockers / Omega-Conotoxin GVIA Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country: