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Pantothenate kinase activation restores brain coenzyme A in a mouse model of pantothenate kinase associated neurodegeneration [Drug Discovery and Translational Medicine]

ASPET

PANK2 is one of three kinases that initiate and regulate coenzyme A biosynthesis from vitamin B5 and the ability of BBP-671, an allosteric activator of pantothenate kinases, to enter the brain and elevate coenzyme A was investigated. Significance Statement The blood brain barrier represents a major hurdle for drugs targeting brain metabolism.

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Pharmacokinetic study of the interaction between luteolin and magnoflorine in rats

Chemical Biology and Drug Design

Magnoflorine increased the systemic exposure and metabolic stability and suppressed the transport of luteolin. Abstract Both luteolin and magnoflorine have been reported to regulate the development of breast cancer, which makes them easier to co-administrate.

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N-glucuronidation: the human element

Metabolite Tales Blog

UGT1A enzymes were shown to be down-regulated in several cancers, and mutations in UGT genes enhance the risk of bladder cancer in smokers [10]. A route to be avoided or a desired route of metabolism? 8(2):3640-3648; [link] [11] Pharmacokinetics of the Multi-kinase Inhibitor Pexidartinib: Mass Balance and Dose Proportionality.

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Tapinarof is a topical aryl hydrocarbon receptor–modulating agent approved for the treatment of psoriasis by downregulating proinflammatory interleukin-17 and regulating expression of the skin-barrier proteins filaggrin and loricrin. Drug metabolism in drug discovery and development. Dermavant’s tapinarof is one such friend.