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-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.
Bowen
Martina E
ME
Department of Chemistry, University of Arizona, Tucson, AZ 85721-0041, USA.
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
D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D005456:Fluorescent Dyes; D007202:Indicators and Reagents; D008024:Ligands; D013058:Mass Spectrometry; D010455:Peptides / Q000138:chemical synthesis*; D011092:Polyethylene Glycols; D015203:Reproducibility of Results; D021241:Spectrometry, Mass, Electrospray Ionization; D000521:alpha-MSH / Q000737:chemistry*
D005456:Fluorescent Dyes; D007202:Indicators and Reagents; D008024:Ligands; D010455:Peptides; D011092:Polyethylene Glycols; D000521:alpha-MSH