某些溴酚对人碳酸酐酶同工酶的影响。
The effects of some bromophenols on human carbonic anhydrase isoenzymes.
作者信息
Taslimi Parham, Gülçin İlhami, Öztaşkın Necla, Çetinkaya Yasin, Göksu Süleyman, Alwasel Saleh H, Supuran Claudiu T
机构信息
a Department of Chemistry , Faculty of Science, Atatürk University , Erzurum , Turkey .
b Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia .
出版信息
J Enzyme Inhib Med Chem. 2016 Aug;31(4):603-7. doi: 10.3109/14756366.2015.1054820. Epub 2015 Jul 2.
Carbonic anhydrases (CAs, EC 4.2.1.1), which are involved in a variety of physiological and pathological processes, are ubiquitous metalloenzymes mainly catalyzing the reversible hydration of carbon dioxide (CO2) to bicarbonate ([Formula: see text]) and proton (H(+)). In this study, a dozen of bromophenol derivatives (1-12) were evaluated as metalloenzyme CA (EC 4.2.1.1) inhibitors against the human carbonic anhydrase isoenzymes I and II (hCA I and II). Cytosolic hCA I and II isoenzymes were effectively inhibited by bromophenol derivatives (1-12) with Kis in the low nanomolar range of 1.85 ± 0.58 to 5.04 ± 1.46 nM against hCA I and in the range of 2.01 ± 0.52 to 2.94 ± 1.31 nM against hCA II, respectively.
碳酸酐酶（CAs，EC 4.2.1.1）参与多种生理和病理过程，是普遍存在的金属酶，主要催化二氧化碳（CO₂）可逆水合形成碳酸氢根（[化学式：见原文]）和质子（H⁺）。在本研究中，评估了十二种溴酚衍生物（1 - 12）作为金属酶碳酸酐酶（EC 4.2.1.1）抑制剂对人碳酸酐酶同工酶I和II（hCA I和II）的抑制作用。溴酚衍生物（1 - 12）有效抑制了胞质hCA I和II同工酶，对hCA I的抑制常数（Ki）在1.85±0.58至5.04±1.46 nM的低纳摩尔范围内，对hCA II的抑制常数在2.01±0.52至2.94±1.31 nM范围内。
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