Supuran Claudiu T
Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Polo Scientifico, Via U. Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Metabolites. 2018 Mar 21;8(2):25. doi: 10.3390/metabo8020025.
Although the role of carbonic anhydrases (CAs, EC 4.2.1.1) in metabolism is well-established, pharmacological applications of this phenomenon started to be considered only recently. In organisms all over the phylogenetic tree, the seven CA genetic families known to date are involved in biosynthetic processes and pH modulation, which may influence metabolism in multiple ways, with both processes being amenable to pharmacologic intervention. CA inhibitors possess antiobesity action directly by inhibiting lipogenesis, whereas the hypoxic tumor metabolism is highly controlled by the transmembrane isoforms CA IX and XII, which contribute to the acidic extracellular environment of tumors and supply bicarbonate for their high proliferation rates. Many of the articles from this special issue deal with the role of cancer CAs in tumor metabolism and how these phenomena can be used for designing innovative antitumor therapies/imaging agents. The metabolic roles of CAs in bacteria and algae are also discussed.
尽管碳酸酐酶(CAs,EC 4.2.1.1)在新陈代谢中的作用已得到充分确立,但直到最近才开始考虑这一现象的药理学应用。在整个系统发育树中的生物体中,迄今已知的七个CA基因家族参与生物合成过程和pH调节,这可能以多种方式影响新陈代谢,并且这两个过程都适合进行药物干预。CA抑制剂通过抑制脂肪生成直接具有抗肥胖作用,而缺氧肿瘤代谢则由跨膜异构体CA IX和XII高度控制,它们有助于肿瘤的酸性细胞外环境,并为其高增殖率提供碳酸氢盐。本期特刊中的许多文章都探讨了癌症CA在肿瘤代谢中的作用,以及如何利用这些现象设计创新的抗肿瘤疗法/成像剂。还讨论了CA在细菌和藻类中的代谢作用。