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参考文献:Anthranilic Acid Based Cck1 Receptor Antagonists: Preliminary Investigation On Their Second "touch Point"
标题:Anthranilic Acid Based Cck1 Receptor Antagonists: Preliminary Investigation On Their Second "touch Point"
摘要:In This Phase Of Structure-Affinity Relationship Study Of Vl-0395,A New Anthranilic Acid Based Cck1 Selective Antagonist,We Propose A Series Of Unnatural Aminoacidic Derivatives. The Result Of This Work Is The Identification Of A New Cck Ligand,Which Possesses An Affinity (Ic50 = 35 Nm) One Order Of Magnitude Greater Than The Lead And,As A General Rule,It Points Out How The Hypothesized Receptorial Pocket Which Accommodates The Phe Residue Allows Much More Structural Modification Than That Interacting With The N-Terminal Group. Hence,The Modification Of The C-Terminal Pharmacophoric Group Of Our Lead Vl-0395 Can Not Only Enhance The Affinity Of Anthranific Acid Derivatives But Can Modulate The Selectivity For One Cck Receptor Subtype Or Afford Mixed Antagonists. (C) 2005 Elsevier Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2005.01.002