Review highlights the development and safety of small molecule glucagon receptor antagonists, indicating potential for glycemic control.
Introduction The glucagon receptor (GCGR) plays a pivotal role in diabetes management. While small molecule GCGR antagonists (GCGRAs) offer several advantages, including glycemic control, oral bioavailability, and cost-effectiveness, their clinical development is hampered by safety concerns. Recent structural and mechanistic insights have elucidated ligand binding and biased signaling and informed the rational design of GCGRAs.
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Wang et al. (2025) studied this question.
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