Heterobivalent ligands crosslink multiple cell-surface receptors: The human melanocortin-4 and δ-opioid receptors

Josef Vagner; Liping Xu; Heather L. Handl; Jatinder S. Josan; David L. Morse; Eugene A. Mash; Robert J. Gillies; Victor J Hruby

doi:10.1002/anie.200702770

Heterobivalent ligands crosslink multiple cell-surface receptors: The human melanocortin-4 and δ-opioid receptors

Josef Vagner, Liping Xu, Heather L. Handl, Jatinder S. Josan, David L. Morse, Eugene A. Mash, Robert J. Gillies, Victor J Hruby

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

66 Scopus citations

Abstract

(Figure Presented) Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and d-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay.

Original language	English (US)
Pages (from-to)	1685-1688
Number of pages	4
Journal	Angewandte Chemie - International Edition
Volume	47
Issue number	9
DOIs	https://doi.org/10.1002/anie.200702770
State	Published - Feb 15 2008

Keywords

Binding assay
Fluorescence spectroscopy
Molecular dynamics
Peptidomimetics
Solid-phase synthesis

ASJC Scopus subject areas

Catalysis
General Chemistry

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10.1002/anie.200702770

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title = "Heterobivalent ligands crosslink multiple cell-surface receptors: The human melanocortin-4 and δ-opioid receptors",

abstract = "(Figure Presented) Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and d-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay.",

keywords = "Binding assay, Fluorescence spectroscopy, Molecular dynamics, Peptidomimetics, Solid-phase synthesis",

author = "Josef Vagner and Liping Xu and Handl, {Heather L.} and Josan, {Jatinder S.} and Morse, {David L.} and Mash, {Eugene A.} and Gillies, {Robert J.} and Hruby, {Victor J}",

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T1 - Heterobivalent ligands crosslink multiple cell-surface receptors

T2 - The human melanocortin-4 and δ-opioid receptors

AU - Vagner, Josef

AU - Xu, Liping

AU - Handl, Heather L.

AU - Josan, Jatinder S.

AU - Morse, David L.

AU - Mash, Eugene A.

AU - Gillies, Robert J.

AU - Hruby, Victor J

PY - 2008/2/15

Y1 - 2008/2/15

N2 - (Figure Presented) Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and d-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay.

AB - (Figure Presented) Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and d-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay.

KW - Binding assay

KW - Fluorescence spectroscopy

KW - Molecular dynamics

KW - Peptidomimetics

KW - Solid-phase synthesis

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Heterobivalent ligands crosslink multiple cell-surface receptors: The human melanocortin-4 and δ-opioid receptors

Abstract

Keywords

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