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公开(公告)号：US20080254442A1
公开(公告)日：2008-10-16
申请号：US11787237
申请日：2007-04-13
CPC分类号： C12N9/78 , C07K2299/00 , C07K2319/21 , C12Y305/01088 , G01N2333/978 , G01N2500/04 , G01N2500/20
摘要： The present invention provides the three-dimensional structure of human mitochondrial Homo sapiens peptide deformylase (HsPDF) protein, and HsPDF complexed to a binding compound, such as a PDF inhibitor. This crystallographic information will aid in the identification and development of novel binding compounds of HsPDF and other PDF family members which have anti-bacterial, anti-viral, anti-parasitical, anti-inflammatory, and/or anti-cancer activity.
摘要翻译： 本发明提供人类线粒体智人肽脱甲酰酶（HsPDF）蛋白质的三维结构和与结合化合物如PDF抑制剂复合的HsPDF。 这种晶体学信息将有助于鉴定和开发具有抗细菌，抗病毒，抗寄生，抗炎和/或抗癌活性的HsPDF和其他PDF家族成员的新型结合化合物。
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2.发明授权Method of inhibitor design and identification using a 3-D structure of human peptide deformylase 有权使用人肽脱甲酰酶的3-D结构的抑制剂设计和鉴定方法公开(公告)号：US07747395B2
公开(公告)日：2010-06-29
申请号：US11787237
申请日：2007-04-13
CPC分类号： C12N9/78 , C07K2299/00 , C07K2319/21 , C12Y305/01088 , G01N2333/978 , G01N2500/04 , G01N2500/20
摘要： The present invention provides the three-dimensional structure of human mitochondrial Homo sapiens peptide deformylase (HsPDF) protein, and HsPDF complexed to a binding compound, such as a PDF inhibitor. This crystallographic information will aid in the identification and development of novel binding compounds of HsPDF and other PDF family members which have anti-bacterial, anti-viral, anti-parasitical, anti-inflammatory, and/or anti-cancer activity.
摘要翻译： 本发明提供人类线粒体智人肽脱甲酰酶（HsPDF）蛋白质的三维结构和与结合化合物如PDF抑制剂复合的HsPDF。 这种晶体学信息将有助于鉴定和开发具有抗细菌，抗病毒，抗寄生，抗炎和/或抗癌活性的HsPDF和其他PDF家族成员的新型结合化合物。
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3.发明授权公开(公告)号：US09056857B2
公开(公告)日：2015-06-16
申请号：US13140741
申请日：2009-12-21
申请人： Lei Zhu , Yueming Li
发明人： Lei Zhu , Yueming Li
IPC分类号： A61K31/55 , A61K31/381 , C07D409/12 , A61K31/5513 , C07D333/34
CPC分类号： A61K31/5513 , A61K31/381 , C07D333/34 , C07D409/12
摘要： Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: where X, R1, R2, subscript m, subscript n and subscript v are as defined herein.
摘要翻译： 提供治疗或预防神经退行性疾病的方法，其包括向具有神经变性疾病的受试者施用有效量的式I化合物：其中X，R 1，R 2，下标m，下标n和下标v如本文所定义。
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公开(公告)号：US20070184488A1
公开(公告)日：2007-08-09
申请号：US11523507
申请日：2006-09-19
申请人： Stephen Brady , James Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules Shafer , Xiaoting Tang
发明人： Stephen Brady , James Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules Shafer , Xiaoting Tang
CPC分类号： C12Q1/37 , C07K7/06 , C07K14/4711 , C12P21/06 , G01N33/6896 , G01N2500/00
摘要： The present invention provides synthetic β-secretase peptide substrates useful in various assays for measuring β-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
摘要翻译： 本发明提供用于测量β-分泌酶活性的各种测定中的合成β-分泌酶肽底物。 公开了在各种测定中识别合成底物和抗体应用的抗体。 本文所公开的肽底物的水解速度明显快于从其中衍生出底物序列的瑞典突变体APP。
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5.发明授权Assays using amyloid precursor proteins with modified β-secretase cleavage sites to monitor β-secretase activity 失效测定使用具有修饰的β-分泌酶切割位点的淀粉样蛋白前体蛋白以监测β-分泌酶活性公开(公告)号：US07196163B2
公开(公告)日：2007-03-27
申请号：US10427208
申请日：2003-04-30
申请人： Daria Jean Hazuda , Elizabeth Chen Dodson , Ming-Tain Lai , Min Xu , Xiao-Ping Shi , Adam J. Simon , Guoxin Wu , Yueming Li , Bruce Register
发明人： Daria Jean Hazuda , Elizabeth Chen Dodson , Ming-Tain Lai , Min Xu , Xiao-Ping Shi , Adam J. Simon , Guoxin Wu , Yueming Li , Bruce Register
CPC分类号： C07K7/06 , A01K2217/05 , A01K2267/0306 , A61K38/00 , C07K5/1016 , C07K5/1019 , C07K5/1021 , C07K14/4711 , C07K16/18 , C12P21/06 , C12Q1/37 , G01N33/5088 , G01N33/6896 , G01N2500/00 , G01N2800/52
摘要： Provided are methods of identifying inhibitors of β-secretase that employ modified β-secretase substrates. The modified β-secretase substrates have β-secretase cleavage sites that are altered from wild type. The amino acid sequences of the altered β-secretase cleavage sites contain different amino acids in at least one of the positions P2-P1-P1′-P2′ of the β-secretase cleavage site. Many of the modified β-secretase substrates are more efficient substrates for β-secretase than are corresponding substrates having wild-type sequences, that is, these modified substrates are more susceptible to enzymatic breakdown by β-secretase. Recombinant polynucleotide molecules encoding the modified β-secretase substrates are provided. Antibodies that recognize cleavage products of the modified β-secretase substrates are provided. Stable cell lines expressing the modified β-secretase substrates are provided. Transgenic animals expressing the modified β-secretase substrates are provided.
摘要翻译： 提供了鉴定使用修饰的β-分泌酶底物的β-分泌酶抑制剂的方法。 修饰的β-分泌酶底物具有从野生型改变的β-分泌酶切割位点。 改变的β-分泌酶切割位点的氨基酸序列在β-分泌酶切割位点的至少一个位置P2-P1-P1'-P2'中含有不同的氨基酸。 许多修饰的β-分泌酶底物比具有野生型序列的相应底物更有效的β-分泌酶底物，也就是说，这些修饰的底物更易受β-分泌酶的酶分解。 提供了编码经修饰的β-分泌酶底物的重组多核苷酸分子。 提供了识别修饰的β-分泌酶底物的切割产物的抗体。 提供了表达改良的β-分泌酶底物的稳定细胞系。 提供了表达改良的β-分泌酶底物的转基因动物。
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公开(公告)号：US20110143954A2
公开(公告)日：2011-06-16
申请号：US12776141
申请日：2010-05-07
申请人： Christopher Shelton , Yuan Tian , Yueming Li
发明人： Christopher Shelton , Yuan Tian , Yueming Li
IPC分类号： G01N33/573 , C12Q1/37 , C12P21/06 , C12N9/99 , C12N5/02 , C40B30/04 , C07K14/47 , C07K7/06 , C07H21/04
CPC分类号： G01N33/573 , C07K14/4711 , G01N33/542 , G01N2333/4709 , G01N2333/948 , G01N2500/02 , G01N2800/2814 , G01N2800/2821
摘要： Polypeptide substrates based on modifications or fragments of the various APP isoforms, assay methods based on the use of these substrates, and screening methods directed toward identifying inhibitors of γ-secretase activity. The assay methods and the screening methods are adapted for use in high throughput multi-well plate assay apparatuses. In many embodiments the substrate polypeptides are labeled for ease of detection, and/or may bind specific ligands that themselves are labeled. Generally the labels promote high specificity as well as high sensitivity of detection. These features render the assay and screening methods that employ the labeled substrates especially suited for use in high throughput assay formats. This disclosure further identifies small polypeptides based on a subsequence motif of Aβ that are shown herein to be potent inhibitors of the activity of γ-secretase.
摘要翻译： 基于各种APP同种型的修饰或片段的多肽底物，基于这些底物的使用的测定方法以及用于鉴定γ-分泌酶活性抑制剂的筛选方法。 测定方法和筛选方法适用于高通量多孔板测定装置。 在许多实施方案中，底物多肽被标记以便于检测，和/或可以结合其本身被标记的特异性配体。 通常，标记物具有高度的特异性和高灵敏度的检测。 这些特征使得使用标记底物的测定和筛选方法特别适用于高通量测定形式。 本公开进一步基于A＆bgr的亚序列基序识别小多肽; 这在本文中显示为γ-分泌酶活性的有效抑制剂。
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公开(公告)号：US07479372B2
公开(公告)日：2009-01-20
申请号：US11523507
申请日：2006-09-19
申请人： Stephen F. Brady , James E. Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules A. Shafer , Xiaoting Tang
发明人： Stephen F. Brady , James E. Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules A. Shafer , Xiaoting Tang
IPC分类号： G01N33/53
CPC分类号： C12Q1/37 , C07K7/06 , C07K14/4711 , C12P21/06 , G01N33/6896 , G01N2500/00
摘要： The present invention provides synthetic β-secretase peptide substrates useful in various assays for measuring β-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
摘要翻译： 本发明提供用于测量β-分泌酶活性的各种测定中的合成β-分泌酶肽底物。 公开了在各种测定中识别合成底物和抗体应用的抗体。 本文所公开的肽底物的水解速度明显快于从其中衍生出底物序列的瑞典突变体APP。
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公开(公告)号：US06753410B2
公开(公告)日：2004-06-22
申请号：US09797820
申请日：2001-03-02
申请人： Alan John Nadin , Joseph George Neduvelil , Mohinder K. Sardana , Jules A. Shafer , Stephen J. Gardell , Ming-Tain Lai , Yueming Li , Bruce D. Dorsey , Dennis C. Dean
发明人： Alan John Nadin , Joseph George Neduvelil , Mohinder K. Sardana , Jules A. Shafer , Stephen J. Gardell , Ming-Tain Lai , Yueming Li , Bruce D. Dorsey , Dennis C. Dean
IPC分类号： C07K508
CPC分类号： C07K5/0207 , A61K38/00 , A61K38/55
摘要： The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or prevention of diseases in which the beta-amyloid peptide is involved, such as Alzheimer's disease.
摘要翻译： 本发明涉及化合物和药物组合物，其包含作为γ-分泌酶抑制剂的化合物，其可用于治疗或预防涉及β-淀粉样蛋白肽的疾病，例如阿尔茨海默氏病。
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公开(公告)号：US20130158017A1
公开(公告)日：2013-06-20
申请号：US13140741
申请日：2009-12-21
申请人： Lei Zhu , Yueming Li
发明人： Lei Zhu , Yueming Li
IPC分类号： C07D409/12 , C07D333/34
CPC分类号： A61K31/5513 , A61K31/381 , C07D333/34 , C07D409/12
摘要： Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: where X, R1, R2, subscript m, subscript n and subscript v are as defined herein.
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公开(公告)号：US20110257027A2
公开(公告)日：2011-10-20
申请号：US12776141
申请日：2010-05-07
申请人： Christopher Shelton , Yuan Tian , Yueming Li
发明人： Christopher Shelton , Yuan Tian , Yueming Li
IPC分类号： G01N33/573 , C12P21/06 , C12N9/99 , C07H21/04 , C40B30/04 , C07K14/47 , C07K7/06 , C12Q1/37 , C12N5/02
CPC分类号： G01N33/573 , C07K14/4711 , G01N33/542 , G01N2333/4709 , G01N2333/948 , G01N2500/02 , G01N2800/2814 , G01N2800/2821
摘要： Polypeptide substrates based on modifications or fragments of the various APP isoforms, assay methods based on the use of these substrates, and screening methods directed toward identifying inhibitors of γ-secretase activity. The assay methods and the screening methods are adapted for use in high throughput multi-well plate assay apparatuses. In many embodiments the substrate polypeptides are labeled for ease of detection, and/or may bind specific ligands that themselves are labeled. Generally the labels promote high specificity as well as high sensitivity of detection. These features render the assay and screening methods that employ the labeled substrates especially suited for use in high throughput assay formats. This disclosure further identifies small polypeptides based on a subsequence motif of Aβ that are shown herein to be potent inhibitors of the activity of γ-secretase.
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