ArticleFrontiers in pharmacology2025
Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators.
Article in Frontiers in pharmacology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
1 citing paper in PubMed.
- Novel Squaramides and Squaramates Containing a Five-Membered Heterocyclic Ring: Synthesis, Structure, and Cytotoxicity.International journal of molecular sciences · 2026Article
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Authors and funding
9 authors.
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Abstract
Targeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds). These antagonists likely bind to a conserved intracellular pocket that is also targeted by the well-known CXCR2 antagonist, navarixin. However, unlike navarixin, the MVH compounds are derived from a completely distinct chemotype, raising the possibility that they may engage the receptor differently and produce biased inhibition of downstream signaling pathways. To deduce these potential biased properties, the compounds were investigated using two NanoBRET-based assays, showing a preferential inhibition of CXCR2-mediated β-arrestin recruitment over G protein activation. Furthermore, a detailed statistical analysis revealed an additional bias in the inhibition profiles dependent on the specific ELR+ chemokine used to stimulate the receptor. Altogether, these results describe the MVH compounds as the first set of biased CXCR2 intracellular antagonists.
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