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G. Hjortø

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Open access Sep 2026

Non-canonical cleavage of GPR125/ADGRA3 releases extracellular receptor fragments detectable in cerebrospinal fluid

Summary Adhesion G protein-coupled receptors (aGPCRs) are crucial for barrier tissues and typically autoproteolytically cleaved into N- and C-terminal fragments (NTF and CTF) that remain non-covalently associated until separation is triggered. Here, we show that human GPR125 (ADGRA3), expressed in choroid plexus epithe...

Anna L. S. Walser, O. Larsen, Chiara Stüdle et al. · 0 citations
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. · 0 citations

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