Discovery, Synthesis, and Structure-Activity Relationships of Conotoxins

Kalyana B Akondi (1, 2) , Markus Muttenthaler (1) , Sébastien Dutertre (3) , Quentin Kaas (1) , David J Craik (1) , Richard J Lewis (1) , Paul F Alewood (1)

1 Institute of Molecular Bioscience
2 Institute for Research in Biomedicine
3 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]

Peptide therapeutics are acclaimed as a promising addition to the pharmaceutical arena, and they continue to attract interest due to their high potency, bioavailability, and fewer concerns with toxicity, drug to drug cross-reactions, and tissue accumulation.1,2 Although poor drug delivery and low in vivo stability are still issues to be addressed, peptides look poised to play an important role in the treatment of diseases ranging from Alzheimer's disease to cancer.2,3 The huge biodiversity offered by venom peptides, specially conotoxins isolated from the venom of predatory marine snails, holds enormous promise for the development of peptide-based drugs.

Domaines: Chimie organique

Kalyana B Akondi, Markus Muttenthaler, Sébastien Dutertre, Quentin Kaas, David J Craik, et al.. Discovery, Synthesis, and Structure-Activity Relationships of Conotoxins. Chemical Reviews, 2014, epub ahead of print. ⟨10.1021/cr400401e⟩. ⟨hal-00982890⟩