一种基于荧光的 p38α 募集位点结合物检测法：鉴定罗匹尼罗为新型 p38α 激酶抑制剂。
A fluorescence-based assay for p38α recruitment site binders: identification of rooperol as a novel p38α kinase inhibitor.
机构信息
Department of Cell Biology, Harvard Medical School, 240 Longwood Ave, Boston, MA 02115, USA.
出版信息
Chembiochem. 2013 Jan 2;14(1):66-71. doi: 10.1002/cbic.201200529. Epub 2012 Dec 6.
Abstract
A new p38α inhibitor: Using a D-recruitment site (DRS) probe for p38α which exploits covalent interaction with Cys119 and alkyne-azide "click" chemistry to identify small molecules that recognize the p38α DRS, the anti-inflammatory natural product rooperol was identified as a novel p38α inhibitor.
摘要
一种新的 p38α 抑制剂：利用一种针对 p38α 的 D-募集位点（DRS）探针，该探针利用与半胱氨酸 119 的共价相互作用和炔基-叠氮化物“点击”化学来识别识别 p38α DRS 的小分子，抗炎天然产物罗泊醇被鉴定为一种新型的 p38α 抑制剂。
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