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4. A solanesol-derived scaffold for multimerization of bioactive peptides

Author

Alleti, Ramesh, Rao, Venkataramanarao, Liping Xu, Gillies, Robert J., and Mash, Eugene A.

Subjects
Azides -- Structure, Azides -- Chemical properties, Ligand binding (Biochemistry) -- Analysis, Peptides -- Structure, Peptides -- Chemical properties, Biological sciences, Chemistry
Abstract

A flexible molecular scaffold bearing varying numbers of terminal alkyne groups is prepared in five steps from solanesol and R(CO)-MSH(4)-N[H.sub.2] ligands are prepared by solid phase synthesis and are N-terminally acylated with 6-azidohexanoic acid. In a competitive binding assay with a Eu-labeled probe based on the superpotent ligand NDP-[alpha]-MSH, the monovalent and multivalent constructs are bound to human melanocortin 4 receptor (hMC4R) as monovalent species.

Published
2010

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