缺氧激活肿瘤相关碳酸酐酶IX酸化细胞外pH的能力。
Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH.
作者信息
Svastová Eliska, Hulíková Alzbeta, Rafajová Monika, Zat'ovicová Miriam, Gibadulinová Adriana, Casini Angela, Cecchi Alessandro, Scozzafava Andrea, Supuran Claudiu T, Pastorek Jaromír, Pastoreková Silvia
机构信息
Centre of Molecular Medicine, Institute of Virology, Slovak Academy of Sciences, Dúbravská cesta 9, 845 05 Bratislava, Slovak Republic.
出版信息
FEBS Lett. 2004 Nov 19;577(3):439-45. doi: 10.1016/j.febslet.2004.10.043.
Acidic extracellular pH (pHe) is a typical attribute of a tumor microenvironment, which has an impact on cancer development and treatment outcome. It was believed to result from an accumulation of lactic acid excessively produced by glycolysis. However, metabolic profiles of glycolysis-impaired tumors have revealed that CO2 is a significant source of acidity, thereby indicating a contribution of carbonic anhydrase (CA). The tumor-associated CA IX isoform is the best candidate, because its extracellular enzyme domain is highly active, expression is induced by hypoxia and correlates with poor prognosis. This study provides the first evidence for the role of CA IX in the control of pHe. We show that CA IX can acidify the pH of the culture medium in hypoxia but not in normoxia. This acidification can be perturbed by deletion of the enzyme active site and inhibited by CA IX-selective sulfonamides, which bind only to hypoxic cells containing CA IX. Our findings suggest that hypoxia regulates both expression and activity of CA IX in order to enhance the extracellular acidification, which may have important implications for tumor progression.
酸性细胞外pH值(pHe)是肿瘤微环境的一个典型特征,它对癌症的发展和治疗结果有影响。人们曾认为这是由糖酵解过度产生的乳酸积累所致。然而,糖酵解受损肿瘤的代谢谱显示,二氧化碳是酸度的一个重要来源,从而表明碳酸酐酶(CA)起到了作用。肿瘤相关的CA IX同工型是最佳候选者,因为其细胞外酶结构域具有高活性,其表达由缺氧诱导,且与不良预后相关。本研究首次提供了CA IX在控制pHe方面作用的证据。我们发现,CA IX在缺氧条件下可使培养基的pH值酸化,但在常氧条件下则不会。这种酸化可因酶活性位点的缺失而受到干扰,并被仅与含有CA IX的缺氧细胞结合的CA IX选择性磺胺类药物所抑制。我们的研究结果表明,缺氧调节CA IX的表达和活性,以增强细胞外酸化,这可能对肿瘤进展具有重要意义。