Mapping Motion: Intermediate States, Deorphanization & Discovery

GPCR News
May 22
2 min read

GPCR Colleagues & Curiosity-Driven Minds,

We’re starting with exciting Dr. GPCR updates: sharpen your skills with our new on-demand course, Techniques for Effective Lead Optimization with Dr. Terry Kenakin, and catch up on cutting-edge insights through our full library of symposia recordings, now available with your Premium Membership.

We’re also spotlighting breakthroughs that challenge dogma and deepen our view of receptor dynamics, from the surprising discovery that β-arrestin can bind GPCRs without receptor activation, to visualizing intermediate states with triple-color FRET, and deorphanizing targets using the new G(z)ESTY assay.

Meanwhile, the industry is moving fast with AI-powered platforms, bold leadership moves, and strategic biotech collaborations reshaping the drug discovery landscape.

Let’s dig into the dynamics together.

Dr. GPCR Updates

Techniques for Effective Lead Optimization – Master pharmacology on demand

Build stronger drug programs with this four-part course by Dr. Terry Kenakin. Learn the fundamentals of ligand activity, mechanism of action, and GPCR discovery strategy—all at your own pace. This course is included with your Premium membership.

Access the Course

Dr. GPCR Symposia – On-demand talks from GPCR trailblazers

Watch anytime. Learn from the best. Catch up on past Dr. GPCR Symposia and dive into big ideas from top scientists, early-career researchers, and innovators shaping the field. These on-demand sessions are included with your Premium membership.

Explore the Symposia

GPCR Publication Highlights

Arrestin recognizes GPCRs independently of the receptor state. Arrestin2 binds β₁AR without ligand-induced activation, reshaping our understanding of biased signaling.