Скачать или смотреть Orthosteric vs Allosteric Modulation: Expanding Drug Discovery for GPCRs |

GPCR scientists have long realized that targeting just the orthosteric site limits what we can achieve. The challenge is finding ways to modulate these receptors more precisely to improve selectivity, druggability, and translational potential—especially for historically tough targets.

This session focuses on understanding GPCRs as allosteric machines. You’ll see clear mechanistic distinctions between orthosteric and allosteric modulation, how allostery reveals new druggable sites, and what that means for modeling or screening next-generation therapeutics. Probe dependence, saturability, and practical limitations are all brought into the discussion, with special attention to how these insights can sharpen your experiments.

Dr. Terry Kenakin walks through the real-world implications of allosteric modulation, showing how these approaches already inform approved drugs and new discovery strategies. The session is direct and grounded, packed with tools and reasoning you can put to work in your own GPCR research.

Learning Outcomes
Distinguish mechanistic features of orthosteric and allosteric modulation in GPCRs
Interpret experimental data using concepts like probe dependence and saturability
Apply allosteric strategies to advance drug discovery on challenging GPCR targets

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