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

J Org Chem. 2007 Mar 2;72(5):1675-80. doi: 10.1021/jo062276g. Epub 2007 Feb 6.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Chromatography, High Pressure Liquid
  • Drug Design
  • Fluorescent Dyes
  • Indicators and Reagents
  • Ligands
  • Mass Spectrometry
  • Peptides / chemical synthesis*
  • Polyethylene Glycols
  • Reproducibility of Results
  • Spectrometry, Mass, Electrospray Ionization
  • alpha-MSH / chemistry*

Substances

  • Fluorescent Dyes
  • Indicators and Reagents
  • Ligands
  • Peptides
  • Polyethylene Glycols
  • alpha-MSH