Design, Synthesis, and Validation of a Branched Flexible Linker for Bioactive Peptides

A branched flexible linker that incorporates a fluorescent dansyl moiety was synthesized and used to connect two high affinity NDP-α-MSH ligands or two low affinity MSH(4) ligands. The linker was incorporated into the conjugate by solid-phase synthesis. In vitro biological evaluations showed that po...

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Veröffentlicht in:Journal of organic chemistry 2007-03, Vol.72 (5), p.1675-1680
Hauptverfasser: Bowen, Martina E, Monguchi, Yasunari, Sankaranarayanan, Rajesh, Vagner, Josef, Begay, Lucinda J, Xu, Liping, Jagadish, Bhumasamudram, Hruby, Victor J, Gillies, Robert J, Mash, Eugene A
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Sprache:eng
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Zusammenfassung:A branched flexible linker that incorporates a fluorescent dansyl moiety was synthesized and used to connect two high affinity NDP-α-MSH ligands or two low affinity MSH(4) ligands. The linker was incorporated into the conjugate by solid-phase synthesis. In vitro biological evaluations showed that potency of binding to the human melanocortin 4 receptor was not diminished for linker−ligand combinations relative to the corresponding ligand alone.
ISSN:0022-3263
1520-6904
DOI:10.1021/jo062276g