heterotrimeric G protein activity biosensors Marta Lopez-Balastegui, Antonella Di Pizio, Jiafei Mao, Jana Selent, et al. for their research on the Relevance of GPCR dynamics for receptor activation, signalling Principles of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate Selection

work on Highly biased agonism for GPCR ligands via nanobody tethering Elk Kossatz, Michel Bouvier, Jana Selent, et al. for their study on G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate pancreatic polypeptide from a structural, functional, and therapeutic perspective Structural basis for selectivity

Biased signaling frameworks centered on receptor conformations have a structural limitation when selectivity specificity to ligand-stabilized receptor conformations; this framework does not fully account for selectivity SBI-553 at NTSR1 functions as a PAM-agonist for arrestin while modulating G protein selectivity through This session with Kenneth Jacobson and Matteo Pavan examines the structural determinants that make selective the orthosteric pocket, with implications for PAM design across GPCRs How P2Y14 antagonists achieve selectivity

Cheloha builds nanobody-GPCR ligand conjugates that rescue weak peptides, engineer receptor selectivity And can selectivity for one receptor subtype be engineered without redesigning the ligand from scratch Conformation selectivity changes the duration of the signal PTH receptor exists in G-protein coupled Attaching a short PTH fragment to a PTHR1-selective nanobody produces a ligand selective for that subtype ; the same fragment attached to a PTHR2-selective nanobody redirects it entirely.

. << Back to podcast list Strategic Partner(s) Jane Lamerdin and Gaurav Agrawal: Building GPCR Assays About the Guests Jane Lamerdin is VP of R&D at Eurofins DiscoverX, where she oversees development of return of GPCRs 47:40 Physiological relevance as the real bottleneck 53:40 One message: scientists first Selected

Pfleger challenges a silent assumption embedded in most of them: that the time point chosen for each Understanding receptor complexes is where the next layer of selectivity and specificity in drug discovery with angiotensin and CCR2 receptors in cell-based systems, working through the logic of functional selectivity 32:26 Screening receptors in complexes, not in isolation 40:03 When cell biology reached the patient Selected