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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.

Hay on class B GPCRs, RAMPs, and the selectivity problem in CGRP-targeted migraine therapies - what the The Erenumab Selectivity Problem Erenumab, the first monoclonal antibody approved against a GPCR complex are conformational and fine-grained, not structurally obvious, making ligand selectivity considerably , selective ligands, and bimolecular fluorescence complementation in vivo 26:42 Structural data and what Because we don't have selective ligands."

John Streicher on how HSP90 flips direction between brain and spinal cord, why isoform-selective inhibitors Current lines of work include isoform-selective HSP90 inhibition as a strategy for widening the opioid The "brain always wins" problem is solved by isoform selectivity, not by dose. With a non-selective HSP90 inhibitor given systemically, the brain effect dominates and pain relief is The route from "intrathecal only" to "oral pill" runs through isoform selectivity.