首页 | 本学科首页   官方微博 | 高级检索  
     


Anion inhibition studies of a beta carbonic anhydrase from the malaria mosquito Anopheles gambiae
Authors:Daniela Vullo  Leo Syrjänen  Marianne Kuuslahti  Seppo Parkkila  Claudiu T. Supuran
Affiliation:1. Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Sesto Fiorentino (Firenze), Italy;2. Faculty of Medicine and Life Sciences, University of Tampere, Tampere, Finland;3. Fimlab Laboratories Ltd, Tampere, Finland;4. Fimlab Laboratories Ltd, Tampere, Finland;5. Neurofarba Dipartment, Sezione di Scienza Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino (Firenze), Italy
Abstract:An anion inhibition study of the β-class carbonic anhydrase, AgaCA, from the malaria mosquito Anopheles gambiae is reported. A series of simple as well as complex inorganic anions, and small molecules known to interact with CAs were included in the study. Bromide, iodide, bisulphite, perchlorate, perrhenate, perruthenate, and peroxydisulphate were ineffective AgaCA inhibitors, with KIs?>?200?mM. Fluoride, chloride, cyanate, thiocyanate, cyanide, bicarbonate, carbonate, nitrite, nitrate, sulphate, stannate, selenate, tellurate, diphosphate, divanadate, tetraborate, selenocyanide, and trithiocarbonate showed KIs in the range of 1.80–9.46?mM, whereas N,N-diethyldithiocarbamate was a submillimolar AgaCA inhibitor (KI of 0.65?mM). The most effective AgaCA inhibitors were sulphamide, sulphamic acid, phenylboronic acid and phenylarsonic acid, with inhibition constants in the range of 21–84?µM. The control of insect vectors responsible of the transmission of many protozoan diseases is rather difficult nowadays, and finding agents which can interfere with these processes, as the enzyme inhibitors investigated here, may arrest the spread of these diseases worldwide.
Keywords:Carbonic anhydrase  anion  Anopheles gambiae  inhibitor  malaria
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号