发明名称 E2 displacement assay for identifying inhibitors of HPV
摘要 The present invention generally relates to an assay for identifying inhibitors of Human Papillomavirus (HPV), comprising: a) contacting a HPV E2 transactivation domain with a probe to form a E2:probe complex and measuring a signal from said probe to establish a base line level; b) incubating the E2:probe complex with a test compound and measuring the signal from said probe; c) comparing the signal from step b) with the signal from step a); wherein said probe is a compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein R<superscript>1>, A, X, W, Y, R<superscript>3 >and R<superscript>4 >are as defined herein; or a derivative thereof, wherein said derivative is a probe of formula (I) labeled with a detectable label or an affinity tag, wherein wavy lines represent bonds of unspecified stereochemistry; and wherein said signal is selected from: fluorescence, resonance energy transfer, time resolved fluorescence, radioactivity, fluorescence polarization, change in the intrinsic spectral properties, luminescence and plasma-resonance; whereby a modulation in said signal is an indication that said test compound binds to said transactivation domain.
申请公布号 US2003194698(A1) 申请公布日期 2003.10.16
申请号 US20030358790 申请日期 2003.02.05
申请人 BOEHRINGER INGELHEIM (CANADA) LTD. 发明人 WHITE PETER;YOAKIM CHRISTIANE
分类号 G01N33/50;C07D407/12;C07D491/10;C07D495/20;G01N33/15;G01N33/532;G01N33/533;G01N33/534;G01N33/535;G01N33/542;G01N33/566;G01N33/569;G01N33/58;G01N33/60;(IPC1-7):C12Q1/70;C07D451/12;C07D491/12 主分类号 G01N33/50
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