Bioorg Med Chem Lett. 2007 Feb 1;17(3):628-35. Epub 2006 Nov 15.

Carbonic anhydrase activators: L-Adrenaline plugs the active site entrance of isozyme II, activating better isoforms I, IV, VA, VII, and XIV.

Temperini C, Innocenti A, Scozzafava A, Mastrolorenzo A, Supuran CT.

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Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.

Abstract

The activation of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) with L-adrenaline and histamine has been investigated by kinetic and X-ray crystallographic studies. L-Adrenaline behaves as a potent activator of isozyme CA I (activation constant of 90 nM), being a much weaker activator of isozyme CA II (activation constant of 96 microM). Isoforms CA IV, VA, VII, and XIV were activated by L-adrenaline with K(A)s in the range of 36-63 microM. The X-ray crystal structure of the CA II-L-adrenaline adduct revealed that the activator plugs the entrance of the active site cavity, obstructing it almost completely.

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Structures reported by this article

Carbonic Anhydrase Activators: Solution And X-ray Crystallography For The Interaction Of Andrenaline With Various Carbonic Anhydrase Isoforms

PDB: 2HKK

Source: Homo sapiens

Method: X-Ray Diffraction

Resolution: 1.9 Å

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