Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

被引：26

作者：

Cifuentes-Pagano, Eugenia ^{[1
]}

Saha, Jaideep ^{[1
,2
]}

Csanyi, Gabor ^{[1
]}

Al Ghouleh, Imad ^{[1
]}

Sahoo, Sanghamitra ^{[1
]}

Rodriguez, Andres ^{[1
]}

Wipf, Peter ^{[2
,3
]}

Pagano, Patrick J. ^{[1
]}

Skoda, Erin M. ^{[2
]}

机构：

[1] Univ Pittsburgh, Dept Pharmacol & Chem Biol, Vasc Med Inst, Pittsburgh, PA 15260 USA

[2] Univ Pittsburgh, Dept Chem, Ctr Chem Methodol & Lib Dev, Pittsburgh, PA 15261 USA

[3] Univ Pittsburgh, Dept Pharmaceut Sci, Pittsburgh, PA 15260 USA

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 07期

基金：

美国国家卫生研究院;

关键词：

OXIDATIVE STRESS; SUPEROXIDE; ACTIVATION; DISEASE; FAMILY; ROS; DERIVATIVES; EXPRESSION; PROTEINS; ZINC;

D O I：

10.1039/c3md00061c

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

(1SR,4RS)-3,3-Dimethyl-1,2,3,4-tetrahydro-1,4-(epiminomethano)naphthalenes were synthesized in 2-3 steps from commercially available materials and assessed for specificity and effectiveness across a range of Nox isoforms. The N-pentyl and N-methylenethiophene substituted analogs 11g and 11h emerged as selective Nox2 inhibitors with cellular IC50 values of 20 and 32 mu M, respectively.

引用

页码：1085 / 1092

页数：8

共 50 条

[31] Regulation of Neutrophil NADPH Oxidase, NOX2: A Crucial Effector in Neutrophil Phenotype and Function
Paclet, Marie-Helene
Laurans, Salome
Dupre-Crochet, Sophie
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY, 2022, 10
[32] Coupling of 6-phosphogluconate dehydrogenase with NADPH oxidase in neutrophils: Nox2 activity regulation by NADPH availability
Baillet, Athan
Xu, Rang
Grichine, Alexei
Berthier, Sylvie
Morel, Francoise
Paclet, Marie-Helene
FASEB JOURNAL, 2011, 25 (07) : 2333 - 2343
[33] Riboflavin (vitamin B2) deficiency impairs NADPH oxidase 2 (Nox2) priming and defense against Listeria monocytogenes
Schramm, Michael
Wiegmann, Katja
Schramm, Sandra
Gluschko, Alexander
Herb, Marc
Utermoehlen, Olaf
Kroenke, Martin
EUROPEAN JOURNAL OF IMMUNOLOGY, 2014, 44 (03) : 728 - 741
[34] Downregulation of PPARα during Experimental Left Ventricular Hypertrophy is Critically Dependent on Nox2 NADPH Oxidase Signalling
Harvey, Adam P.
Robinson, Emma
Edgar, Kevin S.
McMullan, Ross
O'Neill, Karla M.
Alderdice, Matthew
Amirkhah, Raheleh
Dunne, Philip D.
McDermott, Barbara J.
Grieve, David J.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2020, 21 (12) : 1 - 21
[35] Effects of NADPH Oxidase Isoform-2 (NOX2) Inhibition on Behavioral Responses and Neuroinflammation in a Mouse Model of Neuropathic Pain
Teixeira-Santos, Luisa
Verissimo, Eduardo
Martins, Sandra
Sousa, Teresa
Albino-Teixeira, Antonio
Pinho, Dora
BIOMEDICINES, 2023, 11 (02)
[36] NADPH oxidase 2 (NOX2): A key target of oxidative stress-mediated platelet activation and thrombosis
Fuentes, Eduardo
Gibbins, Jonathan M.
Holbrook, Lisa M.
Palomo, Ivan
TRENDS IN CARDIOVASCULAR MEDICINE, 2018, 28 (07) : 429 - 434
[37] NADPH Oxidase NOX2 Mediates Rapid Cellular Oxidation following ATP Stimulation of Endotoxin-Primed Macrophages
Moore, Samantha F.
MacKenzie, Amanda B.
JOURNAL OF IMMUNOLOGY, 2009, 183 (05) : 3302 - 3308
[38] Role of Putative Second Transmembrane Region of Nox2 Protein in the Structural Stability and Electron Transfer of the Phagocytic NADPH Oxidase
Picciocchi, Antoine
Debeurme, Franck
Beaumel, Sylvain
Dagher, Marie-Claire
Grunwald, Didier
Jesaitis, Algirdas J.
Stasia, Marie-Jose
JOURNAL OF BIOLOGICAL CHEMISTRY, 2011, 286 (32) : 28357 - 28369
[39] Divergent effects of genetic and pharmacological inhibition of Nox2 NADPH oxidase on insulin resistance-related vascular damage
Maqbool, Azhar
Watt, Nicole T.
Haywood, Natalie
Viswambharan, Hema
Skromna, Anna
Makava, Natalia
Visnagri, Asjad
Shawer, Heba M.
Bridge, Katherine
Muminov, Shovkat K.
Griffin, Kathryn
Beech, David J.
Wheatcroft, Stephen B.
Porter, Karen E.
Simmons, Katie J.
Sukumar, Piruthivi
Shah, Ajay M.
Cubbon, Richard M.
Kearney, Mark T.
Yuldasheva, Nadira Y.
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY, 2020, 319 (01): : C64 - C74
[40] Signalling mechanisms underlying doxorubicin and Nox2 NADPH oxidase-induced cardiomyopathy: involvement of mitofusin-2
McLaughlin, Declan
Zhao, Youyou
O'Neill, Karla M.
Edgar, Kevin S.
Dunne, Philip D.
Kearney, Anna M.
Grieve, David J.
McDermott, Barbara J.
BRITISH JOURNAL OF PHARMACOLOGY, 2017, 174 (21) : 3677 - 3695

← 1 2 3 4 5 →