Скачать или смотреть Exploitable GPCR Ligand Behaviors: From Dimerization to Location Bias |

The challenge with GPCR-targeted drugs is that conventional models often miss the true signaling diversity and therapeutic opportunities. Many scientists still view GPCRs as static targets, but the field is changing quickly as more ligand behaviors come into focus.

This session examines how GPCRs form functional heteromers, how partial and super agonism reveal new pharmacological possibilities, and why location bias as well as intracellular signaling add new layers to prediction and design. Central examples include PAM-antagonists, constitutive receptor activity, RAMP modulation, and the potential of targeting receptor complexes for specificity.

Dr. Terry Kenakin draws on the latest research to clarify these concepts with practical detail. You’ll hear how subtle shifts in receptor context and ligand design can guide better candidate selection and may open up therapeutic paths where older approaches have stalled.

Learning Outcomes
Interpret how dimerization and receptor heteromers impact GPCR signaling and selectivity
Apply principles of partial, super, and protean agonism to pharmacological strategy
Assess the implications of location bias and intracellular signaling for next-generation drug targeting

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