Concanamycin A (Folimycin) 是一种多聚环内酯类抗生素,是选择性空泡状 H+-ATP 酶 (V-ATPase) 和溶酶体酸化抑制剂,可用于研究炎症。Concanamycin A 可增强细胞毒性 T 淋巴细胞对受感染原代细胞的免疫清除,抑制来自 HIV 和猿猴免疫缺陷病毒不同分支的 Nef 等位基因,可用于研究HIV 感染。
Concanamycin B is a macrolide antibiotic that selectively inhibits vacuolar type H+-ATPases, also known as V-ATPases (IC50 = 5 nM). In this way, it blocks the acidification of vacuolar organelles as well as early to late endosomal transport. Concanamycin B interferes with bone resorption and maturation of CD8 T lymphocytes. It also prevents processing of major histocompatibility complex (MHC) class II precursors in human B cells, inhibiting the expression of MHC class II molecules on the cell surface.
Concanamycin C, a natural macrolide antibiotic, was initially isolated from Streptomyces and identified as an inhibitor of T-cell proliferation in response to concanavalin A (1,2). It exhibits cytotoxicity to fungi, including yeasts, by inhibiting vacuolar-type ATPases (3,4).