Targeting GRP receptor: Design, synthesis and preliminary biological characterization of new non-peptide antagonists of bombesin
Abstract
• The conformation of Bombesin (BN) in presence of a membrane mimetic is an α-helix. • New non-peptide BN antagonists based on a rigid scaffold are reported. • Their pharmacophores have the same orientation than BN key residues for GRP-R binding. • They inhibit BN-induced Ca 2+ mobilization at nanomolar concentrations. • They inhibit BN-induced PC3 and MCF-7 proliferation at nanomolar concentrations. We report the rational design, synthesis, and...
Paper Details
Title
Targeting GRP receptor: Design, synthesis and preliminary biological characterization of new non-peptide antagonists of bombesin
Published Date
Apr 1, 2021
Journal
Volume
109
Pages
104739 - 104739
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