G protein-coupled receptors (GPCRs) constitute the largest receptor family in the human genome and regulate virtually all known physiological processes. Notably, almost 34% of all marketed drugs target this family of receptors. However, about 85% of the approximately 800 human GPCRs are yet to be successfully exploited for therapeutic purposes. Challenges that account for this restricted targeting include the over 100 orphan GPCRs that lack tools to study their functions and our incomplete understanding of the complex signaling and pharmacology of many GPCRs (i.e., allosteric regulation, inverse agonism, biased signaling). Furthermore, many of the screening strategies currently in use are based on classical GPCR signaling paradigms and are not sufficiently nuanced to address the various dimensions of GPCR signaling.

In this GEN webinar, our expert panelists will introduce bioSensAll™, an enhanced bystander bioluminescence resonance energy transfer (ebBRET)-based biosensor technology that addresses bottlenecks limiting current GPCR drug discovery and development efforts. Through various examples, our presenters will discuss how novel GPCR pharmacology concepts can be revealed by this new biosensor technology to advance drug discovery, expand the current GPCR target space, and ultimately unlock untapped therapeutic potential for this complex class of receptors.

A live Q&A session will follow the presentations, offering you a chance to pose questions to our expert panelists.