Better GPCR Drug Discovery Decisions Start With Structured Learning
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Better GPCR Drug Discovery Decisions Start With Structured Learning


Molecular structures with "Sharper Structure. Smarter Decisions." text. White background, Dr. GPCR logo, and subtle hexagonal patterns.


Strong GPCR drug discovery decisions are built on structure, early risk awareness, and focused signal detection.


If you work in GPCR research, clarity is leverage. The ability to access the right framework, detect risk early, and act on emerging signals determines whether programs accelerate—or stall.


This week’s issue focuses on structure, early safety strategy, and the next wave of signal transduction research. Each piece is designed to help you make better decisions—faster.



🔍 This Week in Premium: Sneak Peek


Industry insights: Confo nominates SSTR5 agonist antibody CFTX-2034; Lilly oral GLP-1 maintenance data; Enveda IND clearance ENV-308; Zealand explores brain-directed obesity therapies.


Upcoming events: 12th Adhesion GPCR Workshop; GPCRnet International Symposium; 5th GPCRs Targeted Drug Discovery Summit.


Career opportunities: Senior Scientist roles; Postdoctoral GPCR positions.


Must-read publications: D2 receptor constitutively active mutants; β2AR allosteric SERS assay; CXCR4 inhibitor burixafor Phase 2.




Dr. GPCR University — Reorganized for Clarity and Speed


The Dr. GPCR University has undergone a structural redesign. This soft launch prioritizes usability and clarity to support stronger GPCR drug discovery decisions across teams.


You can now search courses by level, topic, or instructor. Each course page includes a short trailer, defined learning outcomes, and explicit take-home messages. Full course videos stream directly from the platform, and downloadable resources are available in one place.


Legacy courses will migrate into this format over the coming weeks, with live courses returning in March.


In the meantime, Premium members continue to have full access to the legacy course pages.


Why this matters now:


  • Stop wasting time hunting for relevant training across fragmented platforms.

  • Align your team around structured learning outcomes, not scattered slide decks.

  • Identify the exact knowledge gap slowing your program—and close it efficiently.


All courses remain included in Premium Membership.



Already a Premium Member? Start learning here ➤



Terry’s Corner — Early Safety Assays For Better GPCR Drug Discovery Decisions


Too many discovery programs fail because early safety signals were underestimated—or missed entirely.


In this session, Dr. Terry Kenakin walks through the core early assays that protect your chemistry, budget, and timeline. This is not theory. It is operational pharmacology designed to prevent avoidable setbacks.


Early safety frameworks directly influence GPCR drug discovery decisions, especially when timelines and capital are tight.


What you gain:


  • Detect scaffold liabilities early—hERG inhibition, mutagenicity, and mechanistic red flags.

  • Interpret cytotoxicity data correctly—distinguish transient stress from meaningful off-target damage.

  • Assess hepatotoxicity risk—anticipate reactive metabolites and high-risk drug–drug interactions.


Since launch, Terry’s Corner has expanded to 30+ courses and three live AMAs covering binding, kinetics, efficacy, mechanism, ADME, and experimental design. It delivers repeatable depth far beyond a short-format workshop.


An upcoming live Ask-Me-Anything (AMA) with Dr. Kenakin takes place February 26 at 12:00 PM EST. Subscribe to the free Kenakin Brief Newsletter to join the AMA.


Premium Members get 50%+ discount when they join Terry’s Corner.



GPCRs: Signal Transduction — Volume II (Call for Papers, Deadline March 14)


Signal transduction remains central to understanding GPCR biology across health and disease. A new volume dedicated to GPCR signal transduction invites contributions spanning cellular biochemistry, mechanistic signaling, and translational implications.


Submissions are welcome across formats including Original Research, Reviews, Methods, Perspectives, Hypothesis and Theory, Technology and Code, and more.


This initiative brings together field experts to advance collective understanding of how GPCR-mediated signaling shapes physiology and pathology. Given the pace of mechanistic and structural insight emerging across the field, coordinated scholarly contribution is timely.


Why consider contributing:


  • Position your work within a focused, visible GPCR signaling collection.

  • Contribute to shaping scientific direction in cellular biochemistry.

  • Strengthen field-wide dialogue around signaling mechanisms and dysfunction.





Why Dr. GPCR Premium Membership Gives You an Edge


GPCR science is accelerating across obesity, CNS, oncology, and metabolic disease. More data. More companies. More noise.


Premium Membership filters that complexity — without filtering out what matters.


Each week, you receive curated, signal-focused intelligence: industry developments, classified publications, priority event tracking, curated career opportunities, and full access to Dr. GPCR University courses — now included in Premium.


That means structured, searchable, expert-led training across levels and topics — without additional course fees.


Premium Members also receive a 50%+ discount on Terry’s Corner, unlocking advanced pharmacology depth and live AMAs with Dr. Terry Kenakin at a significantly reduced cost.


This is not commentary. It is structured access and structured education.


Premium supports more confident GPCR drug discovery decisions by helping you:


  • Detect meaningful shifts early — without wading through noise.

  • Strengthen mechanistic understanding through organized expert frameworks.

  • Equip your team with repeatable training resources in one place.

  • Reduce external training spend while increasing scientific depth.


It supports scientists refining expertise. It strengthens teams executing discovery programs. It equips leaders making strategic and capital decisions.


When decisions compound, scattered information creates drag.Structured access creates momentum.


Premium delivers that — consistently.




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