Download MendeleyCarbonic 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, C.T.(2007) Bioorg Med Chem Lett 17: 628-635
- PubMed: 17127057
- DOI: https://doi.org/10.1016/j.bmcl.2006.11.027
- Primary Citation of Related Structures:
2HKK - PubMed 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.
Organizational Affiliation:
Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.
