布鲁顿酪氨酸激酶
类风湿性关节炎
酪氨酸激酶
体外
酪氨酸
体内
加药
计算生物学
化学
医学
生物化学
药理学
免疫学
生物
信号转导
生物技术
作者
Zhengying Pan,Heleen Scheerens,Shyr‐Jiann Li,Brian E. Schultz,Paul A. Sprengeler,Leland C. Burrill,Rohan Mendonca,M. D. Sweeney,Keana C. K. Scott,Paul G. Grothaus,Douglas A. Jeffery,Jill M. Spoerke,Lee Honigberg,Peter R. Young,Stacie A. Dalrymple,James T. Palmer
出处
期刊:ChemMedChem
[Wiley]
日期:2006-12-12
卷期号:2 (1): 58-61
被引量:619
标识
DOI:10.1002/cmdc.200600221
摘要
A series of highly selective irreversible inhibitors for Bruton's tyrosine kinase (Btk) was developed using a structural bioinformatics approach. Their capabilities to modulate Btk's activity were characterized both in vitro and in vivo. Oral treatment with once-a-day dosing of compound 4 greatly inhibited disease development in a rodent rheumatoid arthritis (RA) model. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2452/2007/z600221_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
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