The effects of some bromophenols on human carbonic anhydrase isoenzymes
Tarih
2016Yazar
Taslimi, Parham
Gulcin, Ilhami
Oztaskin, Necla
Cetinkaya, Yasin
Goksu, Suleyman
Alwasel, Saleh H.
Supuran, Claudiu T.
Üst veri
Tüm öğe kaydını gösterÖzet
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 (HCO3-) 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 K-is 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.