Design, Synthesis, and Evaluation of Trihalomethyl Ketone Derivatives of Neocarzilin A as Improved Antimetastatic Agents
Noah M. Moriarty,
Annaleigh M. Benton,
Lauren E. Gartenhaus
et al.
Abstract:Vesicle Amine Transport-1 (VAT1) is a protein that is overexpressed in many cancers, including breast cancer, glioblastoma, and angiosarcoma. High VAT1 expression correlates with poor overall survival, and genetic knockout models of VAT1 indicate potent antimigratory activity, suggesting that VAT1 is a promising antimetastasis target. Recently, the natural product neocarzilin A (NCA) from Streptomyces carzinostaticus was reported to be the first validated small-molecule inhibitor of VAT1, having strong activit… Show more
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