Choosing the Right GPCR Assays for Translational Drug Discovery 180

Episode Summary

Potent in vitro hits often fail in vivo—Martin Marro details how robust assay choice and pathway deconvolution can revive GPCR drug discovery programs.

Listeners will learn practical approaches to assay development for GPCR drug discovery, the pitfalls of calcium readouts, and how identifying pathway bias impacts translational success. Dr. Marro shares his experience bridging in vitro–in vivo gaps, refining selection flowcharts, and leveraging pharmacology research to drive clinical candidates. His strategic perspective is rooted in years of leading multimodal discovery teams in pharma and biotech.

Key Takeaways

• Assay selection critically shapes the trajectory from hit to clinic.
• Calcium and IP1 assays may not predict in vivo efficacy for all Gq-coupled receptor targets
• Alternative pathway analysis may be essential for mechanism elucidation.
• Persistence in probing beyond standard readouts can rescue high-profile discovery programs.
• Team structure and collaborative problem-solving are pivotal in resolving translational bottlenecks.

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About the Guest

Dr. Martin Marro leads the Cell Pharmacology group in the DOCTA division at Lilly’s Seaport Innovation Center in Boston, MA. Trained as a pharmacologist, Dr. Marro has accumulated over 20 years of experience spanning large pharmaceutical firms—including GSK, Novartis, and Lilly—and innovative biotech such as Tectonic Therapeutic. He holds deep expertise in early drug discovery across small molecules, peptides, and antibody therapeutics for metabolic, cardiovascular, and gastrointestinal diseases.

Dr. Marro’s research has been central to the discovery and characterization of multiple clinical candidates, with a focus on GPCR target validation, receptor pharmacology, and translational assay strategies. He played a key role in patenting and developing novel fatty acid-conjugated GLP-1 receptor agonists. Driven by the challenge of translating robust in vitro science into clinical proof-of-concept, Dr. Marro’s leadership continues to impact the field of GPCR drug discovery.

Keywords: gpcr podcast, assay development, pharmacology research.