ArticleActa pharmacologica Sinica2026
Discovery of a potent and orally bioavailable type Ⅰ PRMTs inhibitor for triple-negative breast cancer treatment.
Article in Acta pharmacologica Sinica, 2026. 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
Triple-negative breast cancer (TNBC) remains the most refractory breast cancer subtype because of its high invasiveness, lack of therapeutic targets and heterogeneity. Type I protein arginine methyltransferases (PRMTs) are important epigenetic enzymes that catalyze the methylation of arginine residues in various proteins, playing crucial roles in numerous cellular processes. Targeting type I PRMTs represents a promising strategy for TNBC. In this study we characterized a novel selective type I PRMTs inhibitor, SKLB06489. Compared with the precursor compound SKLB06329 (F = 0.2%), SKLB06489 exhibited a markedly enhanced oral bioavailability (F = 88.4%). SKLB06489 inhibited PRMT1, PRMT6, and PRMT8 with IC
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