Small-molecule inhibitors of NADPH oxidase 4

Gábor Borbély; István Szabadkai; Zoltán Horváth; Péter Markó; Zoltán Varga; Nóra Breza; Ferenc Baska; Tibor Vántus; Mónika Huszár; Miklós Geiszt; László Hunyady; László Buday; László Örfi; György Kéri

doi:10.1021/jm1004368

Small-molecule inhibitors of NADPH oxidase 4

Gábor Borbély, István Szabadkai, Zoltán Horváth, Péter Markó, Zoltán Varga, Nóra Breza, Ferenc Baska, Tibor Vántus, Mónika Huszár, Miklós Geiszt, László Hunyady, László Buday, László Örfi, György Kéri

Research output: Contribution to journal › Article › peer-review

50 Scopus citations

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 language	English (US)
Pages (from-to)	6758-6762
Number of pages	5
Journal	Journal of medicinal chemistry
Volume	53
Issue number	18
DOIs	https://doi.org/10.1021/jm1004368
State	Published - Sep 23 2010
Externally published	Yes

Publisher link

10.1021/jm1004368

Find It

Find It at U of M Libraries

Cite this

@article{21967bc0db5d4d6cacf95f5f01975fea,

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 Zolt{\'a}n Varga and N{\'o}ra Breza and Ferenc Baska and Tibor V{\'a}ntus and M{\'o}nika Husz{\'a}r and Mikl{\'o}s Geiszt and L{\'a}szl{\'o} Hunyady and L{\'a}szl{\'o} Buday and L{\'a}szl{\'o} {\"O}rfi and Gy{\"o}rgy K{\'e}ri",

year = "2010",

month = sep,

day = "23",

doi = "10.1021/jm1004368",

language = "English (US)",

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, Zoltán

AU - Breza, Nóra

AU - Baska, Ferenc

AU - Vántus, Tibor

AU - Huszár, Mónika

AU - Geiszt, Miklós

AU - Hunyady, László

AU - Buday, László

AU - Örfi, László

AU - Kéri, György

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

C2 - 20731357

AN - SCOPUS:77956764327

SN - 0022-2623

VL - 53

SP - 6758

EP - 6762

JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 18

ER -

Small-molecule inhibitors of NADPH oxidase 4

Abstract

Publisher link

Find It

Other files and links

Fingerprint

Cite this