Synthesis and In vitro Biological Activity of Cyclic Lipophilic χ-Conotoxin MrIA Analogues

  title={Synthesis and In vitro Biological Activity of Cyclic Lipophilic $\chi$-Conotoxin MrIA Analogues},
  author={Zoltan Dekan and Filip A. Paczkowski and Richard James Lewis and Paul F. Alewood},
  journal={International Journal of Peptide Research and Therapeutics},
The 13-residue peptide, χ-conotoxin MrIA extracted from the venom of Conus marmoreus, is a potent and selective inhibitor of the human noradrenaline transporter (NET). With the aim of improving its biophysical properties, chemical modifications were performed including the attachment of a lipophilic amino acid at the N-terminus and cyclisation of the peptide backbone with functionality introduced into the linker. All χ-conotoxin MrIA analogues were assembled on solid phase by highly optimised… 

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