Designing allosteric modulators to change GPCR G protein subtype selectivity
2025. 11. 5. 09:40ㆍScience Reports & Study
Moore, M.N., Person, K.L., Robleto, V.L. et al. Designing allosteric modulators to change GPCR G protein subtype selectivity. Nature (2025).
https://doi.org/10.1038/s41586-025-09643-2
RESEARCH BRIEFINGS29 October 2025
Molecular ‘glues’ and ‘bumpers’ on receptors can bias signalling inside the cell
Compounds that bind to the intracellular core of G-protein-coupled receptors can encourage interactions with some G proteins and prevent them with others, leading to a switch in downstream signalling pathways. Rational design of such core-targeted compounds could be used to find small molecules that modulate this diverse superfamily of receptors.