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)

Research output: Contribution to journalArticleScientificpeer-review

9 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

Fingerprint

Carbonic Anhydrases
Amines
Protein Isoforms
Chemical activation
Membranes
Amino Acids
Aromatic Amino Acids
Biogenic Amines
Histamine
Epinephrine
Neurotransmitter Agents
Dopamine
Serotonin
Tissue

Keywords

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

Cite this

Innocenti, Alessio ; Hilvo, Mika ; Parkkila, Seppo ; Scozzafava, Andrea ; Supuran, Claudiu T. / Carbonic anhydrase activators : Activation of the membrane-associated isoform XV with amino acids and amines. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 13. pp. 3430-3433.
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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.",
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Carbonic anhydrase activators : Activation of the membrane-associated isoform XV with amino acids and amines. / Innocenti, Alessio; Hilvo, Mika; Parkkila, Seppo; Scozzafava, Andrea; Supuran, Claudiu T. (Corresponding Author).

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 13, 2009, p. 3430-3433.

Research output: Contribution to journalArticleScientificpeer-review

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T2 - Activation of the membrane-associated isoform XV with amino acids and amines

AU - Innocenti, Alessio

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AU - Scozzafava, Andrea

AU - Supuran, Claudiu T.

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N2 - 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.

AB - 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.

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