Carbonic anhydrase inhibitors: inhibition of the  cytosolic human isozyme VII with anions

Daniela Vullo; Eva Ruusuvuori; Kai Kaila; Andrea Scozzafava; Claudiu T Supuran

doi:10.1016/j.bmcl.2006.03.078

Carbonic anhydrase inhibitors: inhibition of the cytosolic human isozyme VII with anions

Daniela Vullo, Eva Ruusuvuori, Kai Kaila, Andrea Scozzafava, Claudiu T Supuran

Laboratory of Neurobiology

Tutkimustuotos: Artikkelijulkaisu › Artikkeli › Tieteellinen › vertaisarvioitu

Abstrakti

An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme VII (hCA VII) with anions has been conducted. Cyanate, cyanide, and hydrogensulfite were weak hCA VII inhibitors (K(I)s in the range of 7.3-15.2 mM). Cl- and HCO3- showed good inhibitory activity against hCA VII (K(I)s of 0.16-1.84 mM), suggesting that this enzyme is not involved in metabolons with anion exchangers or sodium bicarbonate cotransporters. The best inhibitors were sulfamate, sulfamide, phenylboronic, and phenylarsonic acid (K(I)s of 6.8-12.5 mu M). (c) 2006 Elsevier Ltd. All rights reserved.

Alkuperäiskieli	englanti
Lehti	Bioorganic & Medicinal Chemistry Letters
Vuosikerta	16
Sivut	3139-3143
Sivumäärä	5
ISSN	0960-894X
DOI - pysyväislinkit	https://doi.org/10.1016/j.bmcl.2006.03.078
Tila	Julkaistu - 2006
OKM-julkaisutyyppi	A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä, vertaisarvioitu

Tieteenalat

311 Peruslääketieteet
118 Biotieteet
515 Psykologia

Pääsy asiakirjaan

10.1016/j.bmcl.2006.03.078

Siteeraa tätä

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abstract = "An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme VII (hCA VII) with anions has been conducted. Cyanate, cyanide, and hydrogensulfite were weak hCA VII inhibitors (K(I)s in the range of 7.3-15.2 mM). Cl- and HCO3- showed good inhibitory activity against hCA VII (K(I)s of 0.16-1.84 mM), suggesting that this enzyme is not involved in metabolons with anion exchangers or sodium bicarbonate cotransporters. The best inhibitors were sulfamate, sulfamide, phenylboronic, and phenylarsonic acid (K(I)s of 6.8-12.5 mu M). (c) 2006 Elsevier Ltd. All rights reserved.",

keywords = "311 Basic medicine, 118 Biological sciences, 515 Psychology",

author = "Daniela Vullo and Eva Ruusuvuori and Kai Kaila and Andrea Scozzafava and Supuran, {Claudiu T}",

year = "2006",

doi = "10.1016/j.bmcl.2006.03.078",

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pages = "3139--3143",

journal = "Bioorganic & Medicinal Chemistry Letters",

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TY - JOUR

T1 - Carbonic anhydrase inhibitors

T2 - inhibition of the cytosolic human isozyme VII with anions

AU - Vullo, Daniela

AU - Ruusuvuori, Eva

AU - Kaila, Kai

AU - Scozzafava, Andrea

AU - Supuran, Claudiu T

PY - 2006

Y1 - 2006

N2 - An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme VII (hCA VII) with anions has been conducted. Cyanate, cyanide, and hydrogensulfite were weak hCA VII inhibitors (K(I)s in the range of 7.3-15.2 mM). Cl- and HCO3- showed good inhibitory activity against hCA VII (K(I)s of 0.16-1.84 mM), suggesting that this enzyme is not involved in metabolons with anion exchangers or sodium bicarbonate cotransporters. The best inhibitors were sulfamate, sulfamide, phenylboronic, and phenylarsonic acid (K(I)s of 6.8-12.5 mu M). (c) 2006 Elsevier Ltd. All rights reserved.

AB - An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme VII (hCA VII) with anions has been conducted. Cyanate, cyanide, and hydrogensulfite were weak hCA VII inhibitors (K(I)s in the range of 7.3-15.2 mM). Cl- and HCO3- showed good inhibitory activity against hCA VII (K(I)s of 0.16-1.84 mM), suggesting that this enzyme is not involved in metabolons with anion exchangers or sodium bicarbonate cotransporters. The best inhibitors were sulfamate, sulfamide, phenylboronic, and phenylarsonic acid (K(I)s of 6.8-12.5 mu M). (c) 2006 Elsevier Ltd. All rights reserved.

KW - 311 Basic medicine

KW - 118 Biological sciences

KW - 515 Psychology

U2 - 10.1016/j.bmcl.2006.03.078

DO - 10.1016/j.bmcl.2006.03.078

M3 - Article

SN - 0960-894X

VL - 16

SP - 3139

EP - 3143

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

ER -