公开(公告)号：EP1732906A4

公开(公告)日：2007-11-21

申请号：EP05733551

申请日：2005-03-25

申请人： MERCK & CO INC

发明人： COBURN CRAIG A ,  ESPESETH AMY S ,  STACHEL SHAWN J ,  OLSEN DAVID B ,  HAZUDA DARIA J ,  HOLLOWAY M KATHARINE

IPC分类号： C07D277/60 ,  A61K31/425 ,  A61P31/18 ,  C07D277/40 ,  C07D277/82 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/08 ,  C07D417/14

CPC分类号： C07D417/14 ,  C07D277/40 ,  C07D277/60 ,  C07D277/82 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/08

公开(公告)号：EP1578356A4

公开(公告)日：2007-08-15

申请号：EP03743199

申请日：2003-02-23

申请人： MERCK & CO INC

发明人： ESPESETH AMY S ,  FERRER MARC ,  FLORES OSVALDO A ,  HAZUDA DARIA J ,  INGLESE JAMES ,  MILLER MICHAEL D ,  REGISTER BRUCE ,  SHI XIAO-PING ,  SIMON ADAM J ,  ZUCK PAUL D

IPC分类号： C07K14/47 ,  C12N15/12 ,  C07H21/02 ,  C12N1/20 ,  C12N15/00 ,  C12P21/06

CPC分类号： C07K14/47 ,  C07K14/4702 ,  C07K14/4711 ,  C07K2319/00 ,  C07K2319/50 ,  G01N2500/10

摘要： The present invention provides DNA constructs, genetically engineered host cells, and methods for identifying inhibitors of amyloid precursor protein (APP) processing. The methods provide for the convenient identification, in a single assay, of inhibitors of β-secretase and Ϝ-secretase as well as other forms of APP processing. The methods rely on fusion proteins of APP and transcription factors in which APP processing releases the transcription factors, allowing the transcription factors to activate transcription of a reporter gene. Inhibitors are identified as substances that block or diminish transcription factor release from the fusion protein, thereby causing a diminution of reporter gene readout.