Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation

被引：569

作者：

Lewis, Huw D. ^{[1
]}

Liddle, John ^{[1
]}

Coote, Jim E. ^{[2
]}

Atkinson, Stephen J. ^{[1
]}

Barker, Michael D. ^{[1
]}

Bax, Benjamin D. ^{[2
]}

Bicker, Kevin L. ^{[3
]}

Bingham, Ryan P. ^{[2
]}

Campbell, Matthew ^{[1
]}

Chen, Yu Hua ^{[2
]}

Chung, Chun-Wa ^{[2
]}

Craggs, Peter D. ^{[2
]}

Davis, Rob P. ^{[1
]}

Eberhard, Dirk ^{[4
]}

Joberty, Gerard ^{[4
]}

Lind, Kenneth E. ^{[5
]}

Locke, Kelly ^{[2
]}

Maller, Claire ^{[1
]}

Martinod, Kimberly ^{[6
,7
]}

Patten, Chris ^{[1
]}

Polyakova, Oxana ^{[2
]}

Rise, Cecil E. ^{[5
]}

Ruediger, Martin ^{[2
]}

Sheppard, Robert J. ^{[1
]}

Slade, Daniel J. ^{[3
]}

Thomas, Pamela ^{[2
]}

Thorpe, Jim ^{[2
]}

Yao, Gang ^{[5
]}

Drewes, Gerard ^{[4
]}

Wagner, Denisa D. ^{[6
,8
,9
]}

Thompson, Paul R. ^{[3
]}

Prinjha, Rab K. ^{[1
]}

Wilson, David M. ^{[1
]}

机构：

[1] GlaxoSmithKline, Med Res Ctr, Immunoinflammat Therapy Area, EpiNova DPU, Stevenage, Herts, England

[2] GlaxoSmithKline, Med Res Ctr, Stevenage, Herts, England

[3] Scripps Florida, Scripps Res Inst, Dept Chem, Jupiter, FL USA

[4] A GSK Co, Cellzome GmbH, Heidelberg, Germany

[5] GlaxoSmithKline, ELT Boston Platform Technol & Sci, Waltham, MA USA

[6] Boston Childrens Hosp, Program Cellular & Mol Med, Boston, MA USA

[7] Harvard Univ, Sch Med, Div Med Sci, Grad Program Immunol, Boston, MA 02115 USA

[8] Boston Childrens Hosp, Div Hematol Oncol, Boston, MA USA

[9] Harvard Univ, Sch Med, Dept Pediat, Boston, MA 02115 USA

来源：

NATURE CHEMICAL BIOLOGY | 2015年 / 11卷 / 03期

基金：

美国国家卫生研究院;

关键词：

ARGININE DEIMINASE 4; NEUTROPHIL EXTRACELLULAR TRAPS; TARGET; REFINEMENT; ACTIVATION; SIMILARITY; DESIGN;

D O I：

10.1038/nchembio.1735

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：

PAD4 has been strongly implicated in the pathogenesis of autoimmune, cardiovascular and oncological diseases through clinical genetics and gene disruption in mice. New selective PAD4 inhibitors binding a calcium-deficient form of the PAD4 enzyme have validated the critical enzymatic role of human and mouse PAD4 in both histone citrullination and neutrophil extracellular trap formation for, to our knowledge, the first time. The therapeutic potential of PAD4 inhibitors can now be explored.

引用

页码：189 / +

页数：6

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