Lucarini Laura, Magnelli Lucia, Schiavone Nicola, Crisci Alfonso, Innocenti Alessio, Puccetti Luca, Cianchi Fabio, Peri Sara, Supuran Claudiu T, Papucci Laura, Masini Emanuela
a Department of Neuroscience, Psychiatry and Drug Area and Child Health (NEUROFARBA), Section of Pharmacology and Toxicology and Section of Pharmaceutical Sciences , University of Florence , Florence , Italy.
b Department of Experimental and Clinical Biomedical Sciences "Mario Serio" , University of Florence , Florence , Italy.
J Enzyme Inhib Med Chem. 2018 Dec;33(1):234-240. doi: 10.1080/14756366.2017.1411350.
Carbonic anhydrase (CA, EC 4.2.1.1) IX is regarded as a tumour hypoxia marker and CA inhibitors have been proposed as a new class of antitumor agents, with one such agent in Phase II clinical trials. The expression of some CAs, in particular the isoforms CA IX and CA XII, has been correlated with tumour aggressiveness and progression in several cancers. The aim of this study was to evaluate the possibility that CA IX could represent a marker related to clear cell Renal Cell Carcinoma (ccRCC). Bcl-2 and Bax, and the activity of caspase-3, evaluated in tissue biopsies from patients, were congruent with resistance to apoptosis in ccRCCs with respect to healthy controls, respectively. In the same samples, the CA IX and pro-angiogenic factor VEGF expressions revealed that both these hypoxia responsive proteins were strongly increased in ccRCC with respect to controls. CA IX plasma concentration and CA activity were assessed in healthy volunteers and patients with benign kidney tumours and ccRCCs. CA IX expression levels were found strongly increased only in plasma from ccRCC subjects, whereas, CA activity was found similarly increased both in plasma from ccRCC and benign tumour patients, compared to healthy volunteers. These results show that the plasmatic level of CA IX, but not the CA total activity, can be considered a diagnostic marker of ccRCCs. Furthermore, as many reports exist relating CA IX inhibition to a better outcome to anticancer therapy in ccRCC, plasma levels of CA IX could be also predictive for response to therapy.
碳酸酐酶(CA,EC 4.2.1.1)IX被视为一种肿瘤缺氧标志物,并且碳酸酐酶抑制剂已被提议作为一类新型抗肿瘤药物,其中一种此类药物正处于II期临床试验阶段。一些碳酸酐酶的表达,特别是同工型CA IX和CA XII,已与几种癌症中的肿瘤侵袭性和进展相关。本研究的目的是评估CA IX是否可能代表一种与透明细胞肾细胞癌(ccRCC)相关的标志物。在患者的组织活检中评估的Bcl-2和Bax以及caspase-3的活性,分别与ccRCC相对于健康对照的抗凋亡能力一致。在相同的样本中,CA IX和促血管生成因子VEGF的表达显示,相对于对照,这两种缺氧反应蛋白在ccRCC中均显著增加。在健康志愿者以及患有良性肾肿瘤和ccRCC的患者中评估了CA IX血浆浓度和CA活性。发现仅在ccRCC受试者的血浆中CA IX表达水平显著增加,而与健康志愿者相比,在ccRCC和良性肿瘤患者的血浆中CA活性均同样增加。这些结果表明,CA IX的血浆水平而非CA总活性可被视为ccRCC的诊断标志物。此外,由于有许多报告将CA IX抑制与ccRCC中更好的抗癌治疗结果相关联,CA IX的血浆水平也可能预测治疗反应。