ArticleACS medicinal chemistry letters2025
Terpene-Based Thiazole Hydrazines as Negative Allosteric Modulators of MRGPRX4: In Vitro Evaluation and Binding Site Analysis.
Article in ACS medicinal chemistry letters, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
The human MAS-related G-protein-coupled receptors (MRGPRs) represent a promising therapeutic target for managing chronic itch and pain. Among them, MRGPRX4 is activated by bile acids in dorsal root ganglia (DRG) neurons and contributes to the cholestatic itch. Here, we report the design, synthesis, and in vitro evaluation of a focused library of functionalized terpene-based thiazole hydrazines targeting MRGPRX receptors. Functional assays identified two compounds,
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