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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References
Hauser, A. S., Attwood, M. M., Rask-Andersen, M., Schiöth, H. B. & Gloriam, D. E. Nat. Rev. Drug Discov. 16, 829–842 (2017).
Ortiz Zacarías, N. V., Lenselink, E. B., IJzerman, A. P., Handel, T. M. & Heitman, L. H. Trends Pharmacol. Sci. 39, 547–559 (2018).
Powers, A. S. et al. Nat. Chem. Biol. 19, 805–814 (2023).
Chan, H. C. S., Li, Y., Dahoun, T., Vogel, H. & Yuan, S. Trends Biochem. Sci. 44, 312–330 (2019).
Katritch, V., Cherezov, V. & Stevens, R. C. Trends Pharmacol. Sci. 33, 17–27 (2012).
Kobayashi, K. et al. Nature 618, 1085–1093 (2023).
Baidya, M., Dwivedi, H. & Shukla, A. K. Nat. Struct. Mol. Biol. 24, 500–502 (2017).
Kumari, P., Inoue, A., Chapman, K., Lian, P. & Rosenbaum, D. M. Proc. Natl Acad. Sci. USA 120, e2219569120 (2023).
Mullard, A. Nat. Rev. Drug Discov. 22, 347–348 (2023).
Smith, J. S., Lefkowitz, R. J. & Rajagopal, S. Nat. Rev. Drug Discov. 17, 243–260 (2018).
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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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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DOI: https://doi.org/10.1038/s41594-023-01100-w