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公开(公告)号：EP2208061B1
公开(公告)日：2017-11-08
申请号：EP08834506.1
申请日：2008-09-26
发明人： WALENSKY, Loren, D. , TJANDRA, Nico , GAVATHIOTIS, Evripidis , SUZUKI, Motoshi , BIRD, Gregory, H.
CPC分类号： G01N33/5079 , C07K14/4747 , G01N33/5011 , G01N33/5035 , G01N2510/00
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2.发明公开METHODS AND COMPOSITIONS FOR MODULATING BCL-2 FAMILY POLYPEPTIDES 有权VERFAHREN UND ZUSAMMENSETZUNGEN ZUR MODULATION VON POLYPEPTIDEN DER BCL-2-FAMILIE
公开(公告)号：EP2208061A2
公开(公告)日：2010-07-21
申请号：EP08834506.1
申请日：2008-09-26
发明人： WALENSKY, Loren, D. , TJANDRA, Nico , GAVATHIOTIS, Evripidis , SUZUKI, Motoshi , BIRD, Gregory, H.
CPC分类号： G01N33/5079 , C07K14/4747 , G01N33/5011 , G01N33/5035 , G01N2510/00
摘要： The present invention is based, at least in part, on the identification of a novel active site on BCL-2 family polypeptide such as BAX, which when bound by a compound, modifies the activity of the BCL-2 family polypeptide.
摘要翻译： 本发明至少部分地基于BCL-2家族多肽如BAX上的新活性位点的鉴定，当被化合物结合时，其修饰BCL-2家族多肽的活性。
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公开(公告)号：EP3401684A3
公开(公告)日：2019-01-16
申请号：EP17210306.1
申请日：2009-10-09
IPC分类号： G01N33/68 , C07K14/435 , A61K38/17 , A61P35/00
摘要： The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an α1 helix, α2 helix, a loop between α1-α2, α6 helix, and select residues of α4, α5, and α8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.
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公开(公告)号：EP3401684A2
公开(公告)日：2018-11-14
申请号：EP17210306.1
申请日：2009-10-09
IPC分类号： G01N33/68 , C07K14/435 , A61K38/17 , A61P35/00
CPC分类号： G06F19/12 , A61K38/00 , C07K14/4747 , C40B30/02
摘要： The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an α1 helix, α2 helix, a loop between α1-α2, α6 helix, and select residues of α4, α5, and α8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.
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公开(公告)号：EP2338056A2
公开(公告)日：2011-06-29
申请号：EP09819587.8
申请日：2009-10-09
IPC分类号： G01N33/68 , C07K14/435 , A61K38/17 , A61P35/00
CPC分类号： G06F19/12 , A61K38/00 , C07K14/4747 , C40B30/02
摘要： The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an αl helix, α2 helix, a loop between αl-α2, α.6 helix, and select residues of α4, α.5, and α.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.
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6.发明授权
公开(公告)号：EP2338056B1
公开(公告)日：2018-01-03
申请号：EP09819587.8
申请日：2009-10-09
IPC分类号： G01N33/68 , C07K14/435 , A61K38/17 , A61P35/00
CPC分类号： G06F19/12 , A61K38/00 , C07K14/4747 , C40B30/02
摘要： The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an α1 helix, α2 helix, a loop between α1-α2, α.6 helix, and select residues of α4, α.5, and α.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.
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