Unconventional Ligands in GPCR Drug Discovery: Prodrugs, Biologics, and Beyond |

Описание: GPCR drug discovery is shifting. Relying solely on classic hormones and small molecules no longer captures the complexity or opportunity in targeting these receptors. The expanding ligand toolbox brings new options for specificity, efficacy, and clinical utility.

This session focuses on unconventional ligand types—prodrugs, biologics, irreversible inhibitors, and molecular glues. You'll get a clear look at strategies like antibody-drug conjugates, chaperone screens, and the contrast between “Me Too” drugs and genuine first-in-class innovation. The reasoning centers on translating mechanism into therapeutics and predicting outcomes.

Dr. Terry Kenakin guides the discussion, breaking down how these new ligand classes address long-standing challenges in GPCR pharmacology. You’ll hear real-world considerations in engineering, selectivity, and translational barriers—grounded in both practical data and forward-looking thinking.

Learning Outcomes
Distinguish the opportunities and challenges of using unconventional ligands for GPCR targeting
Evaluate how novel ligand classes impact selectivity and translational outcomes
Interpret the implications of new mechanistic approaches for advancing GPCR therapeutics

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