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Design, synthesis, and validation of a branched flexible linker for bioactive peptides.


ABSTRACT: A branched flexible linker that incorporates a fluorescent dansyl moiety was synthesized and used to connect two high affinity NDP-alpha-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.

SUBMITTER: Bowen ME 

PROVIDER: S-EPMC3538035 | biostudies-literature | 2007 Mar

REPOSITORIES: biostudies-literature

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Design, synthesis, and validation of a branched flexible linker for bioactive peptides.

Bowen Martina E ME   Monguchi Yasunari Y   Sankaranarayanan Rajesh R   Vagner Josef J   Begay Lucinda J LJ   Xu Liping L   Jagadish Bhumasamudram B   Hruby Victor J VJ   Gillies Robert J RJ   Mash Eugene A EA  

The Journal of organic chemistry 20070206 5


A branched flexible linker that incorporates a fluorescent dansyl moiety was synthesized and used to connect two high affinity NDP-alpha-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. ...[more]

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