Title: Discovery of a new class of macrocyclic antagonists to the human motilin receptor
Authors: Marsault, Eric ×
Hoveyda, Hamid R
Peterson, Mark L
Saint-Louis, Carl
Landry, Annick
Vézina, Martin
Ouellet, Luc
Wang, Zhigang
Ramaseshan, Mahesh
Beaubien, Sylvie
Benakli, Kamel
Beauchemin, Sophie
Déziel, Robert
Peeters, Theo
Fraser, Graeme L #
Issue Date: Nov-2006
Series Title: Journal of Medicinal Chemistry vol:49 issue:24 pages:7190-7
Abstract: A novel class of macrocyclic peptidomimetics was identified and optimized as potent antagonists to the human motilin receptor (hMOT-R). Well-defined structure-activity relationships allowed for rapid optimization of potency that eventually led to high affinity antagonists to hMOT-R. Potency and antagonist functional activity were confirmed both in functional and cell-based assays, as well as on isolated rabbit intestinal smooth muscle strips. Rapid access to this novel class of macrocyclic target structures was made possible through two efficient and complementary solid-phase parallel synthetic approaches, both of which are reported herein.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Translational Research in GastroIntestinal Disorders
× corresponding author
# (joint) last author

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