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

Martina E. Bowen; Yasunari Monguchi; Rajesh Sankaranarayanan; Josef Vagner; Lucinda J. Begay; Liping Xu; Bhumasamudram Jagadish; Victor J. Hruby; Robert J. Gillies; Eugene A. Mash

doi:10.1021/jo062276g

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

Martina E. Bowen, Yasunari Monguchi, Rajesh Sankaranarayanan, Josef Vagner, Lucinda J. Begay, Liping Xu, Bhumasamudram Jagadish, Victor J. Hruby, Robert J. Gillies, Eugene A. Mash

Research output: Contribution to journal › Article › peer-review

15 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	1675-1680
Number of pages	6
Journal	Journal of Organic Chemistry
Volume	72
Issue number	5
DOIs	https://doi.org/10.1021/jo062276g
State	Published - Mar 2 2007

ASJC Scopus subject areas

Organic Chemistry

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abstract = "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.",

author = "Bowen, {Martina E.} and Yasunari Monguchi and Rajesh Sankaranarayanan and Josef Vagner and Begay, {Lucinda J.} and Liping Xu and Bhumasamudram Jagadish and Hruby, {Victor J.} and Gillies, {Robert J.} and Mash, {Eugene A.}",

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T1 - Design, synthesis, and validation of a branched flexible linker for bioactive peptides

AU - Bowen, Martina E.

AU - Monguchi, Yasunari

AU - Sankaranarayanan, Rajesh

AU - Vagner, Josef

AU - Begay, Lucinda J.

AU - Xu, Liping

AU - Jagadish, Bhumasamudram

AU - Hruby, Victor J.

AU - Gillies, Robert J.

AU - Mash, Eugene A.

PY - 2007/3/2

Y1 - 2007/3/2

N2 - 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.

AB - 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.

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JO - Journal of Organic Chemistry

JF - Journal of Organic Chemistry

SN - 0022-3263

IS - 5

ER -

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

Abstract

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