α-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters
Yükleniyor...
Tarih
2012
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Carbonic anhydrases (CA) catalyze activated ester hydrolysis in addition to the hydration of CO2 to bicarbonate. They also show phosphatase activity with 4-nitrophenyl phosphate as substrate but not sulfatase with the corresponding sulfate. Here we prove that the enzyme is catalyzing the synthesis of cyclic diols from sulfate esters. 5-, 6-and 8-membered ring cyclic sulfates incorporating a neighboring secondary alcohol moiety were treated with CA II and yielded the corresponding cyclic diols. Inhibitory properties of obtained cyclic and original sulfate esters were then investigated on human carbonic anhydrase I (hCA I), hCA II, hCA IV and hCA VI (h=human isoform). KI-s of these compounds ranged between 32.7423 ?M against hCA I, 2.1332.4 ?M against hCA II, 13.7234 ?M against hCA IV and 76278 ?M against CA VI, respectively. The sulfatase activity of CA with such esters is amazing considering the fact that 4-nitrophenyl-sulfate is not a substrate of these enzymes.
Açıklama
PubMed:22050606
Anahtar Kelimeler
Antiglaucoma, Carbonic Anhydrase, Cyclic Diols, Inhibition
Kaynak
WoS Q Değeri
Q4
Scopus Q Değeri
Q1
Cilt
27
Sayı
1
Künye
Çavdar, H., Ekinci, D., Talaz, O., Saraçoğlu, N., Şentürk, M., Supuran, C. T. (2012). Α-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters. Journal of Enzyme Inhibition and Medicinal Chemistry, 27, 1, 148-154.
