The development of small-moiecule giucagon antagonists reported in the scientific literature is summarized. Peptidic and nonpeptidic giucagon antagonists have been shown to attenuate giucagon-induced glucose production in animal models. To date, various classes of compounds having affinity for the glucagon receptor have been identified. Recently, a competitive human small-molecule glucagon antagonist was reported to block glucagon-stimulated glucose production in humans. Thus, small molecules that antagonize the glucagon receptor are potential therapeutic agents for the control of diabetes.
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Alexander Ling (2002) studied this question.