多种金属酶碳酸酐酶（CA, EC 4.2.1.1）的异构体与肿瘤发生密切相关。由于缺氧肿瘤而导致的HIF激活级联反应使CA IX和XII过度表达，参与PH调节、代谢和转移形成。其他异构体（CA I，II，III，IV）在一些肿瘤中也有报道。一些CA异构体是疾病进展或治疗反应的生物标志物。该文讨论了用于肿瘤/转移治疗的靶向这些酶的抑制剂、抗体和其他方法。磺胺类和香豆素类被视为最常研究的抑制剂类别，但也有人研究了含有羧酸盐、硒和碲的抑制剂。报道了CA抑制剂与其他抗肿瘤药物的混合药物用于多靶点治疗。用选择性、靶向抑制剂靶向实体或血液肿瘤中的CA是一种经过验证的方法，在过去几年已经得到了巩固。大量新的临床前数据和多个抗体和小分子抑制剂的临床试验正在进行中，与大量有效的新化合物/方法相结合，可能在这一治疗领域取得突破。通过从2018年到2023年在PubMed、ScienceDirect、Espacenet和PatentGuru搜索科学和专利文献。

Several isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) are connected with tumorigenesis. Hypoxic tumors overexpress CA IX and XII as a consequence of HIF activation cascade, being involved in pH regulation, metabolism, metastases formation. Other isoforms (CA I, II, III, IV) were also reported to be present in some tumors.Some CA isoforms are biomarkers for diseases progression or response to therapy. Inhibitors, antibodies, and other procedures for targeting these enzymes for the treatment of tumors/metastases are discussed. Sulfonamides and coumarins represent the most investigated classes of inhibitors, but carboxylates, selenium and tellurium-containing inhibitors were also investigated. Hybrid drugs of CA inhibitors with other antitumor agents for multitargeted therapy were reported.Targeting CAs present in solid or hematological tumors with selective, targeted inhibitors is a validated approach, which has been consolidated in the last years. A host of new preclinical data and several clinical trials of antibodies and small molecule inhibitors are ongoing, which connected with the large number of new chemotypes/procedures discovered to be effective, may lead to a breakthrough in this therapeutic area. The scientific/patent literature has been searched for on PubMed, ScienceDirect, Espacenet and PatentGuru, from 2018 to 2023.