碳酸酐酶抑制剂包被的金纳米颗粒对肿瘤相关同工酶IX的抑制作用强于胞质同工酶I和II。
Carbonic anhydrase inhibitor coated gold nanoparticles selectively inhibit the tumor-associated isoform IX over the cytosolic isozymes I and II.
作者信息
Stiti Maamar, Cecchi Alessandro, Rami Marouan, Abdaoui Mohamed, Barragan-Montero Véronique, Scozzafava Andrea, Guari Yannick, Winum Jean-Yves, Supuran Claudiu T
机构信息
Institut des Biomolécules Max Mousseron UMR 5247 CNRS-UM1-UM2 Ecole Nationale Supérieure de Chimie de Montpellier, Montpellier Cedex, France.
出版信息
J Am Chem Soc. 2008 Dec 3;130(48):16130-1. doi: 10.1021/ja805558k.
An approach for the synthesis of carbonic anhydrase (CA, EC 4.2.1.1) inhibitor coated gold nanoparticles is reported. This nanomaterial selectively inhibited the tumor-associated isoform CA IX overexpressed in hypoxic cancers over the ubiquitous, cytosolic housekeeping isozymes CA I and II and was membrane impermeant. As CA IX has an extracellular active site, the new nanomaterial which is confined to the extracellular space may be useful for imaging and treatment of hypoxic tumors.
报道了一种合成碳酸酐酶（CA，EC 4.2.1.1）抑制剂包覆金纳米颗粒的方法。这种纳米材料相较于普遍存在的胞质管家同工酶CA I和CA II，能选择性抑制在缺氧癌症中过表达的肿瘤相关同工酶CA IX，且不能透过细胞膜。由于CA IX具有细胞外活性位点，这种局限于细胞外空间的新型纳米材料可能对缺氧肿瘤的成像和治疗有用。
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