PMID: 8457566Mar 30, 1993Paper

Thermodynamics of binding of the CO2-competitive inhibitor imidazole and related compounds to human carbonic anhydrase I: an isothermal titration calorimetry approach to studying weak binding by displacement with strong inhibitors

Biochemistry
R G KhalifahE S Rowe

Abstract

The visible spectrum of Co(II)-substituted human carbonic anhydrase I (HCA I) complexed with the unique CO2-competitive inhibitor imidazole undergoes a marked alkaline intensification, with a midpoint near pH 8 [Bauer, R., Limkilde, P., & Johansen, J. T. (1977) Carlsberg Res. Commun. 42, 325-339]. This change was first attributed to the ionization of a nondisplaced water ligand of the active-site metal in a five-coordinate complex. Later proposals favored assigning it to the deprotonation of the bound imidazole itself to give a tetrahedrally coordinated imidazolate anion at high pH. We have determined by isothermal titration calorimetry the pH dependence of the enthalpy of binding of imidazole and its analogues to HCA I and Co(II)HCA I. We devised an indirect strategy whereby the enthalpy of binding of the strong sulfonamide inhibitor methazolamide was determined in the absence and presence of a constant high concentration of the competing imidazole or its analogues. The standard enthalpy of binding of deprotonated methazolamide to the "acid" form of HCA I and Co(II)HCA I was found to be pH independent over the pH range of 6.5-9.5, as expected. It was also identical for both the zinc (-13.5 +/- 1.1 kcal M-1) and the cobalt (-13...Continue Reading

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Citations

Jun 9, 2012·BMC Biophysics·Lina Baranauskienė, Daumantas Matulis
Mar 21, 2003·Biophysical Chemistry·Raja G Khalifah
Nov 20, 2012·Bioorganic & Medicinal Chemistry·Vaida JogaitėDaumantas Matulis
Apr 19, 2007·Chemistry, an Asian Journal·Vijay M KrishnamurthyGeorge M Whitesides
Apr 25, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Vaida MorkūnaitėDaumantas Matulis
Jun 12, 2014·Physical Chemistry Chemical Physics : PCCP·Predrag V PetrovićJean-Pierre Djukic
Sep 4, 2004·Journal of Receptor and Signal Transduction Research·Remo PerozzoLeonardo Scapozza
Feb 23, 2021·Journal of Enzyme Inhibition and Medicinal Chemistry·Alessio NocentiniClaudiu T Supuran

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