Linafexor, a pulsatile FXR agonist, effectively treats bile acid-related liver diseases by mimicking natural bile acid signaling cycles, avoiding toxicity linked to continuous activation.
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Drug Transport and Resistance Mechanisms
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A novel small-molecule inverse agonist, HEP-50768, effectively targets MRGPRX4 and suppresses cholestatic itch in preclinical models.
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IMP-2380 effectively inhibits the NorA efflux pump in Staphylococcus aureus, restoring antibiotic susceptibility with low-nanomolar potency and structural trapping of the transporter.
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Duvakitug significantly improved clinical remission rates in patients with moderate to severe ulcerative colitis, with response rates of up to 48% at week 14.
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Molecular regulators and cell interactions make the blood-brain barrier a dynamic, highly selective interface crucial for CNS health and disease.
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Commensal dysbiosis increases primary bile acids by elevated primary BAs in gut microbiome, driving HR+ breast cancer metastasis via PGE2 signaling.
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