Experimental Oncology and Immunology, Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy.
NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Sesto Fiorentino, Florence, Italy.
J Enzyme Inhib Med Chem. 2022 Dec;37(1):280-286. doi: 10.1080/14756366.2021.2004592.
Carbonic anhydrase IX/XII (CA IX/XII), are cell-surface enzymes typically expressed by cancer cells as a form of adaptation to hypoxia and acidosis. It has been widely reported that these proteins play pivotal roles in cancer progression fostering cell migration, aggressiveness and resistance to first line chemo- and radiotherapies. CA IX has emerged as a promising target in cancer therapy and several approaches and families of compounds were characterised in the attempt to find optimal targeting by inhibiting of the high catalytic activity of the enzyme. In the present work, different cell lines representing glioblastoma, bladder and pancreatic cancer have been exploited to compare the inhibitory and antiproliferative effect of primary sulphonamide acetazolamide (AAZ), the Phase Ib/II clinical grade sulphonamide SLC-0111, and a membrane-impermeant positively charged, pyridinium-derivative (C18). New hints regarding the possibility to exploit CA inhibitors in these cancer types are proposed.
碳酸酐酶 IX/XII(CA IX/XII)是一种细胞表面酶,通常在癌细胞中表达,作为对缺氧和酸中毒的适应形式。广泛报道称,这些蛋白质在促进细胞迁移、侵袭性和对一线化疗和放疗的耐药性方面发挥着关键作用。CA IX 已成为癌症治疗的一个有前途的靶点,已经有几种方法和化合物家族被描述,试图通过抑制酶的高催化活性来找到最佳的靶向。在本工作中,利用代表脑胶质瘤、膀胱癌和胰腺癌的不同细胞系,比较了原发性磺酰胺乙酰唑胺(AAZ)、Ib/II 期临床级磺酰胺 SLC-0111 和一种不可渗透膜的正电荷、吡啶鎓衍生物(C18)的抑制和增殖作用。提出了在这些癌症类型中利用 CA 抑制剂的可能性的新线索。