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PDBsum entry 2hkk

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Lyase PDB id
2hkk
Jmol
Contents
Protein chain
256 a.a.
Ligands
ALE
Metals
_ZN
_HG
Waters ×192

References listed in PDB file
Key reference
Title Carbonic anhydrase activators: l-Adrenaline plugs the active site entrance of isozyme ii, Activating better isoforms i, Iv, Va, Vii, And xiv.
Authors C.Temperini, A.Innocenti, A.Scozzafava, A.Mastrolorenzo, C.T.Supuran.
Ref. Bioorg Med Chem Lett, 2007, 17, 628-635. [DOI no: 10.1016/j.bmcl.2006.11.027]
PubMed id 17127057
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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 Headers