Author

Francesco Casartelli

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Open access Jul 2026

Development of Potent G Protein Pathway-Biased GPR183 Agonists

The detailed structure-activity investigations and optimizations led to the identification of full agonists for GPR183 with complete bias for Gαi protein signaling and low nanomolar potency, including 63 (TUG-2604) with potency and efficacy similar to 7α,25-OHC.

Kaustubh R. Bhuskute, Asmita Manandhar, V. M. S. Kjær et al. · bioRxiv · 0 citations