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

doi:10.1016/j.bmcl.2009.05.026

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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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 (K_As 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 language	English
Pages (from-to)	3430-3433
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2009.05.026
Publication status	Published - 2009
MoE publication type	A1 Journal article-refereed

Keywords

Carbonic anhydrase
Isoform XV
Amine
Amino acid
Enzyme activator

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10.1016/j.bmcl.2009.05.026

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

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.",

keywords = "Carbonic anhydrase, Isoform XV, Amine, Amino acid, Enzyme activator",

author = "Alessio Innocenti and Mika Hilvo and Seppo Parkkila and Andrea Scozzafava and Supuran, {Claudiu T.}",

year = "2009",

doi = "10.1016/j.bmcl.2009.05.026",

language = "English",

volume = "19",

pages = "3430--3433",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Carbonic anhydrase activators

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

AU - Innocenti, Alessio

AU - Hilvo, Mika

AU - Parkkila, Seppo

AU - Scozzafava, Andrea

AU - Supuran, Claudiu T.

PY - 2009

Y1 - 2009

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.

KW - Carbonic anhydrase

KW - Isoform XV

KW - Amine

KW - Amino acid

KW - Enzyme activator

U2 - 10.1016/j.bmcl.2009.05.026

DO - 10.1016/j.bmcl.2009.05.026

M3 - Article

SN - 0960-894X

VL - 19

SP - 3430

EP - 3433

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 13

ER -

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

Abstract

Keywords

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