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公开(公告)号：US07785879B1
公开(公告)日：2010-08-31
申请号：US11522698
申请日：2006-09-18
申请人： Wenyan Wang , Shahriar Shane Taremi , Winifred W. Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
发明人： Wenyan Wang , Shahriar Shane Taremi , Winifred W. Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
CPC分类号： C07K14/70567 , C07K14/4705 , C07K2319/31
摘要： The present invention relates, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.
摘要翻译： 本发明尤其涉及PXR多肽和晶体，其可用于例如结晶和用于鉴定PXR调节剂的测定。
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12.发明授权Polynucleotides encoding polypeptide fragments of protein kinase B gamma (AKT3) 失效编码蛋白激酶Bγ（AKT3）多肽片段的多核苷酸公开(公告)号：US07776589B1
公开(公告)日：2010-08-17
申请号：US11847801
申请日：2007-08-30
申请人： Andrew J. Prongay , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
发明人： Andrew J. Prongay , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention provides, in part, AKT3 polypeptides and methods of use thereof along with nucleic acids encoding the polypeptides. For example, methods for screening for AKT3 inhibitors are provided herein.
摘要翻译： 本发明部分地提供AKT3多肽及其与编码多肽的核酸的使用方法。 例如，本文提供了用于筛选AKT3抑制剂的方法。
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公开(公告)号：US08440443B1
公开(公告)日：2013-05-14
申请号：US11749550
申请日：2007-05-16
申请人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
发明人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
IPC分类号： C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00 , C07K2319/40
摘要： The present invention provides, inter alia, crystals of the MEK1 polypeptide which are particularly useful for structure based drug design as well as methods of use thereof.
摘要翻译： 本发明特别提供了特别可用于基于结构的药物设计的MEK1多肽的晶体及其使用方法。
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14.发明申请SOLUBLE, STABLE FORM OF HDM2, CRYSTALLINE FORMS THEREOF AND METHODS OF USE THEREOF 失效可溶性HDM2的稳定形式，其结晶形式及其使用方法公开(公告)号：US20100136620A1
公开(公告)日：2010-06-03
申请号：US12621241
申请日：2009-11-18
申请人： Shahriar Shane Taremi , Gaolian Xie , Thomas Hesson , Jose S. Duca , Corey Strickland , William T. Windsor , Vincent S. Madison , Rumin Zhang , Paul Reichert , Yaolin Wang
发明人： Shahriar Shane Taremi , Gaolian Xie , Thomas Hesson , Jose S. Duca , Corey Strickland , William T. Windsor , Vincent S. Madison , Rumin Zhang , Paul Reichert , Yaolin Wang
CPC分类号： C07H21/04 , C07D209/20 , C07K14/47 , C07K2299/00
摘要： The present invention discloses modified Hdm2 proteins that are soluble. In addition, the present invention discloses nucleic acids that encode the modified Hdm2 proteins of the present invention. The invention also provides crystals of modified Hdm2 proteins that are suitable for X-ray crystallization analysis. The present invention also discloses methods of using the modified Hdm2 proteins and crystals thereof to identify, select and/or design compounds that may be used as anticancer agents. The present invention further discloses compounds that bind to modified Hdm2 proteins in protein-ligand complexes.
摘要翻译： 本发明公开了可溶性的修饰的Hdm2蛋白。 此外，本发明公开了编码本发明的修饰的Hdm2蛋白质的核酸。 本发明还提供了适用于X射线结晶分析的修饰的Hdm2蛋白晶体。 本发明还公开了使用修饰的Hdm2蛋白及其晶体鉴定，选择和/或设计可用作抗癌剂的化合物的方法。 本发明还公开了与蛋白质 - 配体复合物中的修饰的Hdm2蛋白结合的化合物。
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15.发明申请CRYSTALLINE FORM OF THE CATALYTIC DOMAIN OF AURORA 2 KINASE AND METHODS OF USE THEREOF 有权AURORA 2激酶的催化域的结晶形式及其使用方法公开(公告)号：US20090081706A1
公开(公告)日：2009-03-26
申请号：US12184770
申请日：2008-08-01
申请人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
发明人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
CPC分类号： C12N9/12
摘要： The present invention discloses nucleic acids that encode an active human Aurora 2 kinase catalytic domain. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human Aurora 2 kinase catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human Aurora 2 kinase. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human Aurora 2 kinase in structure assisted drug design to identify compounds that can modulate the enzymatic activity of human Aurora 2 kinase.
摘要翻译： 本发明公开了编码活性人Aurora 2激酶催化结构域的核酸。 本发明还公开了生长包含活性人Aurora 2激酶催化结构域的多肽的X射线衍射晶体的方法。 本发明还公开了人Aurora 2激酶的催化结构域的结晶形式。 此外，本发明公开了在结构辅助药物设计中使用人Aurora 2激酶的X射线衍射晶体的方法来鉴定可调节人Aurora 2激酶的酶活性的化合物。
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公开(公告)号：US08710188B2
公开(公告)日：2014-04-29
申请号：US13149011
申请日：2011-05-31
申请人： Brian M. Beyer , Alan W. Hruza , Richard N. Ingram , Vincent S. Madison , Andrew J. Prongay , Paul Reichert
发明人： Brian M. Beyer , Alan W. Hruza , Richard N. Ingram , Vincent S. Madison , Andrew J. Prongay , Paul Reichert
CPC分类号： C12Q1/56 , A61K38/00 , C07K2299/00 , C12N9/644 , C12Y304/21022 , G01N2500/04
摘要： The present invention relates to factor IXa complexes and crystals thereof as well as methods for identifying inhibitors of factor IXa.
摘要翻译： 本发明涉及因子IXa复合物及其晶体，以及鉴定因子IXa抑制剂的方法。
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17.发明授权公开(公告)号：US08048663B2
公开(公告)日：2011-11-01
申请号：US12815817
申请日：2010-06-15
申请人： Wenyan Wang , Shahriar Shane Taremi , Winifred Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
发明人： Wenyan Wang , Shahriar Shane Taremi , Winifred Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
CPC分类号： C07K14/70567 , C07K14/4705 , C07K2319/31
摘要： The present invention relates to Pregnane X receptor (PXR) polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.
摘要翻译： 本发明涉及可用于例如结晶和用于鉴定PXR调节剂的测定中的孕烷X受体（PXR）多肽和晶体。
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公开(公告)号：US20100286372A1
公开(公告)日：2010-11-11
申请号：US12815817
申请日：2010-06-15
申请人： Wenyan Wang , Shahriar Shane Taremi , Winifred Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
发明人： Wenyan Wang , Shahriar Shane Taremi , Winifred Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
IPC分类号： C07K14/00
CPC分类号： C07K14/70567 , C07K14/4705 , C07K2319/31
摘要： The present invention relates, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.
摘要翻译： 本发明尤其涉及PXR多肽和晶体，其可用于例如结晶和用于鉴定PXR调节剂的测定。
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19.发明授权公开(公告)号：US07824491B2
公开(公告)日：2010-11-02
申请号：US12184770
申请日：2008-08-01
申请人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
发明人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
CPC分类号： C12N9/12
摘要： The present invention discloses nucleic acids that encode an active human Aurora 2 kinase catalytic domain. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human Aurora 2 kinase catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human Aurora 2 kinase. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human Aurora 2 kinase in structure assisted drug design to identify compounds that can modulate the enzymatic activity of human Aurora 2 kinase.
摘要翻译： 本发明公开了编码活性人Aurora 2激酶催化结构域的核酸。 本发明还公开了生长包含活性人Aurora 2激酶催化结构域的多肽的X射线衍射晶体的方法。 本发明还公开了人Aurora 2激酶的催化结构域的结晶形式。 此外，本发明公开了在结构辅助药物设计中使用人Aurora 2激酶的X射线衍射晶体的方法来鉴定可调节人Aurora 2激酶的酶活性的化合物。
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公开(公告)号：US20100267053A1
公开(公告)日：2010-10-21
申请号：US12784760
申请日：2010-05-21
申请人： ANDREW J. PRONGAY , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
发明人： ANDREW J. PRONGAY , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention provides, in part, AKT3 polypeptides and methods of use thereof along with nucleic acids encoding the polypeptides. For example, methods for screening for AKT3 inhibitors are provided herein.
摘要翻译： 本发明部分地提供AKT3多肽及其与编码多肽的核酸的使用方法。 例如，本文提供了用于筛选AKT3抑制剂的方法。
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