Carbonic anhydrase activators: Activation of the membrane-associated isoform XV with amino acids and amines

Alessio Innocenti, Mika Hilvo, Seppo Parkkila, Andrea Scozzafava, Claudiu T. Supuran (Corresponding Author)

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10 Citations (Scopus)

Abstract

An activation study of the membrane-associated carbonic anhydrase (CA, EC 4.2.1.1) isoform XV with a series of natural and non-natural amino acids and aromatic/heterocyclic amines is reported. Murine CA XV was strongly activated by some amino acids (d-Phe, l-/d-DOPA, d-Trp, l-Tyr) and amines (dopamine, serotonin, l-adrenaline and 4-(2-aminoethyl)-morpholine) with activation constants in the range of 4.0–9.5 μM. l-/d-His, l-Phe, histamine and several other heterocyclic amines showed less efficient activation (KAs in the range of 11.6–33.4 μM). The activation profile of CA XV is quite different from that of the cytosolic isoforms CA I and II or the membrane-associated CA IV. All mammalian isoforms CA I–XV are thus characterized for their interaction with this set of amino acid and amine activators, some of which are biogenic amines or neurotransmitters present in sufficiently high amounts in various tissues for exerting significant biologic responses.
Original languageEnglish
Pages (from-to)3430-3433
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number13
DOIs
Publication statusPublished - 2009
MoE publication typeA1 Journal article-refereed

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Keywords

  • Carbonic anhydrase
  • Isoform XV
  • Amine
  • Amino acid
  • Enzyme activator

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