Anacardic acid (AA) was first detected in the shells of cashew nuts, Anacardium occidentale, and is known to possess inhibitory activity against acetyltransferases. Recently, several anacardic acid derivatives (AAds) were isolated from the wild fungus, Tyromyces fissilis, which has been reported as xanthine oxidase inhibitors. In the present study, we investigated whether nine AAds function as acetyltransferase inhibitors.
View Article and Find Full Text PDFS100A9, a multifunctional protein mainly expressed by neutrophils and monocytes, poses an immunological paradox. In virus infections or sterile inflammation, it functions as an alarmin attracting innate immune cells, as well as mediating proinflammatory effects through TLR4 signaling. However, in cancer, S100A9 levels have been shown to associate with poor prognosis and lack of response to immunotherapy.
View Article and Find Full Text PDFClinical studies have shown that inhibitors of bromodomain and extra-terminal domain (BET) proteins, particularly BRD4, have antitumor activity and efficacy. The BET protein has two domains, BD1 and BD2, and we previously focused on BD1 and reported orally bioavailable BD1-selective inhibitors. In this study, we obtained a BD1 inhibitor, a more potent and highly selective pyrazolopyridone derivative 13a, and confirmed its in vivo efficacy.
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