Small-molecule inhibitors of NADPH oxidase 4

Gábor Borbély, István Szabadkai, Zoltán Horváth, Péter Markó, Z. Varga, Nóra Breza, Ferenc Baska, T. Vántus, Mónika Huszár, M. Geiszt, L. Hunyady, L. Buday, L. Őrfi, G. Kéri

Research output: Contribution to journalArticle

41 Citations (Scopus)

Abstract

NOX enzymes are the major contributors in many oxidative damage related diseases. Unfortunately, at present no specific NOX inhibitor is available. Here, we describe the discovery and development of novel NOX4 inhibitors. Compound libraries were tested in a cell-based assay as a primary screen, monitoring H2O2 production. Twenty-four compounds inhibited Nox4 activity with low-micromolar IC50 values of which three were selected for further drug development.

Original languageEnglish
Pages (from-to)6758-6762
Number of pages5
JournalJournal of Medicinal Chemistry
Volume53
Issue number18
DOIs
Publication statusPublished - Sep 23 2010

Fingerprint

NADPH Oxidase
Inhibitory Concentration 50
Libraries
Enzymes
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery
  • Medicine(all)

Cite this

Borbély, G., Szabadkai, I., Horváth, Z., Markó, P., Varga, Z., Breza, N., ... Kéri, G. (2010). Small-molecule inhibitors of NADPH oxidase 4. Journal of Medicinal Chemistry, 53(18), 6758-6762. https://doi.org/10.1021/jm1004368

Small-molecule inhibitors of NADPH oxidase 4. / Borbély, Gábor; Szabadkai, István; Horváth, Zoltán; Markó, Péter; Varga, Z.; Breza, Nóra; Baska, Ferenc; Vántus, T.; Huszár, Mónika; Geiszt, M.; Hunyady, L.; Buday, L.; Őrfi, L.; Kéri, G.

In: Journal of Medicinal Chemistry, Vol. 53, No. 18, 23.09.2010, p. 6758-6762.

Research output: Contribution to journalArticle

Borbély, G, Szabadkai, I, Horváth, Z, Markó, P, Varga, Z, Breza, N, Baska, F, Vántus, T, Huszár, M, Geiszt, M, Hunyady, L, Buday, L, Őrfi, L & Kéri, G 2010, 'Small-molecule inhibitors of NADPH oxidase 4', Journal of Medicinal Chemistry, vol. 53, no. 18, pp. 6758-6762. https://doi.org/10.1021/jm1004368
Borbély G, Szabadkai I, Horváth Z, Markó P, Varga Z, Breza N et al. Small-molecule inhibitors of NADPH oxidase 4. Journal of Medicinal Chemistry. 2010 Sep 23;53(18):6758-6762. https://doi.org/10.1021/jm1004368
Borbély, Gábor ; Szabadkai, István ; Horváth, Zoltán ; Markó, Péter ; Varga, Z. ; Breza, Nóra ; Baska, Ferenc ; Vántus, T. ; Huszár, Mónika ; Geiszt, M. ; Hunyady, L. ; Buday, L. ; Őrfi, L. ; Kéri, G. / Small-molecule inhibitors of NADPH oxidase 4. In: Journal of Medicinal Chemistry. 2010 ; Vol. 53, No. 18. pp. 6758-6762.
@article{ba5d79640f4f4e0abdea9122a15a7524,
title = "Small-molecule inhibitors of NADPH oxidase 4",
abstract = "NOX enzymes are the major contributors in many oxidative damage related diseases. Unfortunately, at present no specific NOX inhibitor is available. Here, we describe the discovery and development of novel NOX4 inhibitors. Compound libraries were tested in a cell-based assay as a primary screen, monitoring H2O2 production. Twenty-four compounds inhibited Nox4 activity with low-micromolar IC50 values of which three were selected for further drug development.",
author = "G{\'a}bor Borb{\'e}ly and Istv{\'a}n Szabadkai and Zolt{\'a}n Horv{\'a}th and P{\'e}ter Mark{\'o} and Z. Varga and N{\'o}ra Breza and Ferenc Baska and T. V{\'a}ntus and M{\'o}nika Husz{\'a}r and M. Geiszt and L. Hunyady and L. Buday and L. Őrfi and G. K{\'e}ri",
year = "2010",
month = "9",
day = "23",
doi = "10.1021/jm1004368",
language = "English",
volume = "53",
pages = "6758--6762",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "18",

}

TY - JOUR

T1 - Small-molecule inhibitors of NADPH oxidase 4

AU - Borbély, Gábor

AU - Szabadkai, István

AU - Horváth, Zoltán

AU - Markó, Péter

AU - Varga, Z.

AU - Breza, Nóra

AU - Baska, Ferenc

AU - Vántus, T.

AU - Huszár, Mónika

AU - Geiszt, M.

AU - Hunyady, L.

AU - Buday, L.

AU - Őrfi, L.

AU - Kéri, G.

PY - 2010/9/23

Y1 - 2010/9/23

N2 - NOX enzymes are the major contributors in many oxidative damage related diseases. Unfortunately, at present no specific NOX inhibitor is available. Here, we describe the discovery and development of novel NOX4 inhibitors. Compound libraries were tested in a cell-based assay as a primary screen, monitoring H2O2 production. Twenty-four compounds inhibited Nox4 activity with low-micromolar IC50 values of which three were selected for further drug development.

AB - NOX enzymes are the major contributors in many oxidative damage related diseases. Unfortunately, at present no specific NOX inhibitor is available. Here, we describe the discovery and development of novel NOX4 inhibitors. Compound libraries were tested in a cell-based assay as a primary screen, monitoring H2O2 production. Twenty-four compounds inhibited Nox4 activity with low-micromolar IC50 values of which three were selected for further drug development.

UR - http://www.scopus.com/inward/record.url?scp=77956764327&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=77956764327&partnerID=8YFLogxK

U2 - 10.1021/jm1004368

DO - 10.1021/jm1004368

M3 - Article

VL - 53

SP - 6758

EP - 6762

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 18

ER -