Basic Information
ID: ALA1134597
Journal: J Med Chem
Title: Identification of alkylidene hydrazides as glucagon receptor antagonists.
Authors: Ling A, Hong Y, Gonzalez J, Gregor V, Polinsky A, Kuki A, Shi S, Teston K, Murphy D, Porter J, Kiel D, Lakis J, Anderes K, May J, Knudsen LB, Lau J.
Abstract: High throughput screening of our small molecule combinatorial library identified a class of benzoylnaphthalenehydrazones with modest affinity for the human glucagon receptor. Optimization of this initial hit through a series of targeted libraries and traditional medicinal chemistry led to ligands with nanomolar affinities. Pharmacological evaluation demonstrated that these ligands were competitive glucagon receptor antagonists. Intravenous administration of a representative benzoylnaphthalenehydrazone into rats attenuated glucagon-stimulated glucose levels.
CiteXplore: 11543683
DOI: 10.1021/jm000547o
Patent ID: ┄
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