Thermodynamic, kinetic, and structural parameterization of human carbonic anhydrase interactions toward enhanced inhibitor design
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چکیده
منابع مشابه
Human carbonic anhydrase III: structural and kinetic study of catalysis and proton transfer.
The residue phenylalanine 198 (Phe 198) is a prominent cause of the lower activity of human carbonic anhydrase III (HCA III) compared with HCA II and other isozymes which have leucine at this site. We report the crystal structures of HCA III and the site-directed mutant F198L HCA III, both at 2.1 A resolution, and the enhancement of catalytic activity by exogenous proton donors containing imida...
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Objective: The present study was carried out to study the binding interactions of different N’-(substituted phenyl sulfonyl)-pyridine-2carbohydrazide derivatives and N’-(substituted phenyl sulfonyl)-thiophene-2-carbohydrazide derivatives which were synthesized by senior students from research laboratory, with objective to explore the suitability of selected ligands for their binding affinity fo...
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The carbonic anhydrase activity of human platelets was investigated by measuring the kinetics of CO2 hydration in supernatants of platelet lysates by using a pH stopped-flow apparatus. An average carbonic anhydrase concentration of 2.1 microM was determined for pellets of human platelets. Analysis of the kinetic properties of this carbonic anhydrase yielded a Km value of 1.0 mM, a catalytic-cen...
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REINHART HEINRICH, §, FRANCISCO MONTERO, ¶, EDDA KLIPP, §, THOMAS G. WADDELL,~ and ENRIQUE MELI~NDEZ-HEVIAt § Humboldt-Universitat zu Berlin, Institut for Biologie, Theoretische Biophysik, D-I 0115 Berlin, Germany ¶ Universidad Complutense de Madrid, Departamento de Bioquimica, 28040 Madrid, Spain ~:University of Tennessee, Department of Chemistry, Chattanooga, TN, USA. tUmversidad de la Laguna...
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Carbonic anhydrases (CAs) are zinc-containing metalloenzymes that catalyze the interconversion of carbon dioxide and bicarbonate. The alpha-class CAs are found predominantly in vertebrates, but they are also expressed in insects like mosquitoes. Recently, an alpha-CA from the midgut of Aedes aegypti larvae (AaCA1) was identified, cloned, and subsequently shown to share high sequence homologous ...
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ژورنال
عنوان ژورنال: Quarterly Reviews of Biophysics
سال: 2018
ISSN: 0033-5835,1469-8994
DOI: 10.1017/s0033583518000082