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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 Dr. GPCR Mission: Dr. GPCR is a scientist-led nonprofit focused on advancing GPCR science through shared rigor, education, and authentic collaboration. Dr. GPCR University extends this mission by creating a common learning space for the global GPCR community—so we all move the field forward together. Unlock full access to all Masterclasses and Premium resources: 👉 https://www.ecosystem.drgpcr.com/gpcr... 🧠 Want more like this? Join the Dr. GPCR Premium Ecosystem to unlock exclusive episodes, practical toolkits, and early access to GPCR University content. 👉 https://www.ecosystem.drgpcr.com/gpcr... _____ Join Terry’s Corner today! Visit https://www.terrykenakin.com for expert-led, on-demand pharmacology courses, and join us at the monthly AMAs with Dr. Terry Kenakin. https://www.ecosystem.drgpcr.com/terr... _____ Get to know our Partner: 👉 Celtarys Research • Company Page: https://www.ecosystem.drgpcr.com/celt... • Press Release: https://www.ecosystem.drgpcr.com/post... • Celtarys News: https://www.ecosystem.drgpcr.com/gpcr... Dr. GPCR is dedicated to fostering a collaborative ecosystem focused on GPCRs. By connecting researchers, sharing knowledge, and facilitating partnerships, the #DrGPCR Ecosystem provides resources to advance GPCR drug discovery. The ecosystem encompasses a range of initiatives to inform and engage the scientific community, including courses, news updates, and networking opportunities.