Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1548-50. doi: 10.1016/j.bmcl.2010.01.081. Epub 2010 Jan 21.
An inhibition study of the transmembrane carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX, XII (tumor-associated), and XIV with anions such as stannate(IV), selenate(VI), tellurate(VI), perosmate(VIII), persulfate, pyrophosphate(V), pyrovanadate(V), tetraborate, persulfate, perrhenate(VII), perrutenate(VII), selenocyanate, iminodisulfonate, fluorosulfate, and trithiocarbonate is reported. Selenate, perosmate, and pyrophosphate were ineffective inhibitors, whereas most of these anions inhibited the three enzymes in the millimolar-submillimolar range. Trithiocarbonate and diethyldithiocarbamate were the best CA IX inhibitors (K(I)s of 1.4-9.7microM), but trithiocarbonate showed less affinity for CA XII and XIV (K(I)s of 0.12-0.66mM). N,N-Diethyldithiocarbamate was a low micromolar inhibitor also against CA XII and XIV (K(I)s of 1.0-1.1microM), suggesting that this new zinc-binding group (CS2-) may lead to efficient inhibitors targeting transmembrane CAs.
报道了阴离子（如锡酸盐(IV)、硒酸盐(VI)、碲酸盐(VI)、过氧代硫酸盐(VIII)、过硫酸盐、焦磷酸盐(V)、焦钒酸盐(V)、四硼酸盐、过硫酸盐、高铼酸盐(VII)、高钌酸盐(VII)、硒氰酸盐、亚氨基二磺酸盐、氟硫酸根和三硫代碳酸根）对跨膜碳酸酐酶（CA，EC 4.2.1.1）同工酶 IX、XII（肿瘤相关）和 XIV 的抑制研究。硒酸盐、过氧代硫酸盐和焦磷酸盐没有抑制作用，而大多数这些阴离子在毫摩尔亚毫摩尔范围内抑制了三种酶。三硫代碳酸根和二乙二硫代氨基甲酸盐是 CAIX 的最佳抑制剂（K（I）为 1.4-9.7μM），但三硫代碳酸根对 CAXII 和 XIV 的亲和力较低（K（I）为 0.12-0.66mM）。N，N-二乙二硫代氨基甲酸盐也是 CAXII 和 XIV 的低微摩尔抑制剂（K（I）为 1.0-1.1μM），表明这种新的锌结合基团（CS2-）可能会导致针对跨膜 CA 的有效抑制剂。
