Pharmacological properties of SD-282 -: An α-isoform selective inhibitor for p38 MAP kinase

被引：9

作者：

Koppelman, Bruce ^{[1
]}

Webb, Heather K. ^{[1
,2
]}

Medicherla, Satyanarayana ^{[1
,3
]}

Almirez, Ramona ^{[1
,4
]}

Feng, Ying ^{[1
]}

Chavez, Jose Carlos ^{[1
]}

Mao, Cheng Ping ^{[1
]}

Nguyen, Aaron ^{[7
]}

Liu, Yu-Wang ^{[1
,4
]}

Kapoun, Ann M. ^{[1
,5
]}

Muiru, Gladys ^{[1
]}

Huang, Yuanying Anne ^{[1
]}

Dugar, Sundeep ^{[1
,9
]}

Mavunkel, Babu J. ^{[1
]}

Lim, Don W. ^{[1
]}

Chakravarty, Sarvajit ^{[1
,6
]}

Luedtke, Gregory ^{[1
,9
]}

Protter, Andrew A. ^{[1
,6
]}

Higgins, Linda S. ^{[1
,8
]}

机构：

[1] Scios Inc, Fremont, CA USA

[2] Arete Therapeut, Hayward, CA USA

[3] Schering Plough Biopharma, Palo Alto, CA USA

[4] Alza, Mountain View, CA USA

[5] Oncomed Pharmaceut, Redwood City, CA USA

[6] Medivat Inc, San Francisco, CA USA

[7] Pharmion Corp, San Francisco, CA USA

[8] InteKrin Therapeut, Los Altos, CA USA

[9] Sai Life Sci Ltd, Hyderabad, Andhra Pradesh, India

来源：

PHARMACOLOGY | 2008年 / 81卷 / 03期

关键词：

p38 MAP kinase; inflammation; cytokine; asthma; sepsis;

D O I：

10.1159/000112865

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of small-molecule p38 inhibitors in numerous models of different disease states have been published, including those of SD-282, an indole-5-carboxamide inhibitor. The aim of the present study was to evaluate the pharmacological activity of SD-282 on cytokine production in vitro as well as in 2 in vivo models of inflammation in order to illuminate the role of this particular inhibitor in diverse disease states. The results presented here provide further characterization of SD-282 and provide a context in which to interpret the activity of this p38 inhibitor in models of arthritis, pain, myocardial injury, sepsis and asthma; all of which have an inflammatory component. SD-282 represents a valuable tool to elucidate the role of p38 MAP kinase in multiple models of inflammation. Copyright (C) 2008 S. Karger AG, Basel.

引用

页码：204 / 220

页数：17

共 76 条

[51] P38 mitogen activated protein kinase regulates endothelial VCAM-1 expression at the post-transcriptional level [J].