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GPCR inhibitors

Structural insights into an intracellular biased agonist for GPCRs

The targeting and modulation of G-protein-coupled receptors (GPCRs) has immense therapeutic potential. A study in Nature now reports on the successful targeting of intracellular allosteric sites that effectively bias GPCR signaling, which has opened new opportunities to develop safer therapeutic agents.

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Fig. 1: Structural details of PTH1R–ligand interactions.

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Acknowledgements

The research program in M.B.’s laboratory is supported by the India Alliance DBT Wellcome Trust (IA/E/20/1/505691) and the Institute Seed Grant (SGT-100081) Indian Institute of Technology Jammu.

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Correspondence to Mithu Baidya.

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Soni, N., Das, T. & Baidya, M. Structural insights into an intracellular biased agonist for GPCRs. Nat Struct Mol Biol 30, 1612–1614 (2023). https://doi.org/10.1038/s41594-023-01100-w

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