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1. 发明公开

EP0873361A4 NUCLEAR RECEPTOR LIGANDS AND LIGAND BINDING DOMAINS 失效
标题翻译：核受体配体和配体结合结构域
公开(公告)号：EP0873361A4
公开(公告)日：2002-10-23
申请号：EP96945800
申请日：1996-12-13
申请人： UNIV CALIFORNIA
发明人： SCANLAN THOMAS S , BAXTER JOHN D , FLETTERICK ROBERT J , WAGNER RICHARD L , KUSHNER PETER J , APRILETTI JAMES L , WEST BRIAN L , SHIAU ANDREW K
IPC分类号： A61K45/00 , A61K31/00 , A61K31/19 , A61K31/192 , A61K31/195 , A61P3/00 , A61P3/06 , A61P5/00 , A61P5/14 , C07K1/00 , C07K14/47 , C07K14/72 , G01N33/48 , G01N33/483 , G01N33/68 , G06F17/50
CPC分类号： C07K14/72 , C07K2299/00

2. 发明公开

EP1297175A4 METHODS AND COMPOUNDS FOR MODULATING NUCLEAR RECEPTOR COACTIVATOR BINDING 审中-公开
标题翻译：方法和化合物调制核受体AM共激活因子的结合
公开(公告)号：EP1297175A4
公开(公告)日：2005-02-02
申请号：EP01950770
申请日：2001-06-29
申请人： UNIV CALIFORNIA
发明人： GUY RODNEY K , BAXTER JOHN D , DARIMONT BEATRICE , FENG WEIJUN , FLETTERICK ROBERT J , KUSHNER PETER J , WAGNER RICHARD L , WEST BRIAN L , YAMAMOTO KEITH R , GEISTLINGER TIMOTHY R , ARNOLD JAMES R , KUNTZ IRWIN D
IPC分类号： C07B61/00 , C07D209/82 , C07D209/88 , C07D225/08 , C07D403/06 , C07D403/14 , C07K1/04 , C07K7/08 , C07K7/56 , G01N33/68 , G06F19/16 , G06F19/18 , C12Q1/00 , A61K38/04 , B01J19/00 , C07K5/00 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/567
CPC分类号： C07D403/06 , C07D209/82 , C07D209/88 , C07D225/08 , C07D403/14 , C07K1/047 , C07K7/08 , C07K7/56 , C07K2299/00 , C40B40/00 , G01N33/6875 , G06F19/16 , G06F19/18
摘要： The present invention relates to methods and agonist/antagonist compounds for modulating nuclear receptor coactivator binding. The invention includes a method for identifying residues comprising a coactivator binding site for a nuclear receptor of interest. Also included is a method of identifying agonists and/or antagonists that bind to a coactivator binding site of a nuclear receptor of interest. Agonists and antagonists of coactivator binding to nuclear receptors also are provided. The invention is exemplified by identification and manipulation of the coactivator binding site of the thyroid receptor (TR), and compounds that bind to this sites. The methods can be applied to other nuclear receptors including RAR, RXR, PPAR, VDR, ER, GR, PR, MR, and AR.

3. 发明专利

CA2240024A1 NUCLEAR RECEPTOR LIGANDS AND LIGAND BINDING DOMAINS 未知
公开(公告)号：CA2240024A1
公开(公告)日：1997-06-19
申请号：CA2240024
申请日：1996-12-13
申请人： UNIV CALIFORNIA
发明人： FLETTERICK ROBERT J , SCANLAN THOMAS S , BAXTER JOHN D , SHIAU ANDREW K , WAGNER RICHARD L , WEST BRIAN L , KUSHNER PETER J , APRILETTI JAMES L
IPC分类号： A61K45/00 , A61K31/00 , A61K31/19 , A61K31/192 , A61K31/195 , A61P3/00 , A61P3/06 , A61P5/00 , A61P5/14 , C07K1/00 , C07K14/47 , C07K14/72 , G01N33/48 , G01N33/483 , G01N33/68 , G06F17/50
摘要： The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three-dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as "TR"). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.

4. 发明申请

WO0061634A3 ECOTIN-VARIANT MODULATORS OF SERINE PROTEASES 审中-公开
标题翻译：丝氨酸蛋白酶的变体调节剂
公开(公告)号：WO0061634A3
公开(公告)日：2001-03-08
申请号：PCT/US0009790
申请日：2000-04-12
申请人： UNIV CALIFORNIA , CRAIK CHARLES S , FLETTERICK ROBERT J
发明人： CRAIK CHARLES S , FLETTERICK ROBERT J
IPC分类号： C07K14/81 , C12N15/31 , G01N33/68
CPC分类号： C07K14/811
摘要： This invention provides a class binding proteins that specifically bind to polypeptides having a chymotrypsin fold (e.g. serine proteases). When the target polypeptides are serine proteases the binding proteins can act to inhibit or activate the serine protease. The binding proteins are based on the structure of ecotin. It was discovered that modification of the amino or carboxyl terminus and/or randomization of one or more of loops 50s, 60s, 80s or 100s will provide an ecotin variant library from which can be selected binding molecules (e.g. protease modulators) specific to virtually any serine protease. Depending on the ecotin variant and the target serine protease, the modulator can act as a serine protease inhibitor or as a serine protease activator. Specific agonists of Factor IXa are disclosed.
摘要翻译：本发明提供了与具有胰凝乳蛋白酶折叠的多肽（例如丝氨酸蛋白酶）特异性结合的类结合蛋白。当靶多肽是丝氨酸蛋白酶时，结合蛋白可起到抑制或激活丝氨酸蛋白酶的作用。结合蛋白是基于生物素的结构。已发现氨基或羧基末端的修饰和/或一个或多个环50s，60s，80s或100s的随机化将提供生物素变体文库，可以从其中选择特异于实际上任何的结合分子（例如蛋白酶调节剂）丝氨酸蛋白酶。根据生物素变体和靶丝氨酸蛋白酶，调节剂可以作为丝氨酸蛋白酶抑制剂或丝氨酸蛋白酶活化剂。公开了因子IXa的特异性激动剂。

5. 发明申请

WO0202488A9 METHODS AND COMPOUNDS FOR MODULATING NUCLEAR RECEPTOR COACTIVATOR BINDING 审中-公开
标题翻译：调节核受体辅助诱导剂结合的方法和化合物
公开(公告)号：WO0202488A9
公开(公告)日：2003-09-12
申请号：PCT/US0120969
申请日：2001-06-29
申请人： UNIV CALIFORNIA
发明人： GUY RODNEY K , BAXTER JOHN D , DARIMONT BEATRICE , FENG WEIJUN , FLETTERICK ROBERT J , KUSHNER PETER J , WAGNER RICHARD L , WEST BRIAN L , YAMAMOTO KEITH R , GEISTLINGER TIMOTHY R , ARNOLD JAMES R , KUNTZ IRWIN D
IPC分类号： C07B61/00 , C07D209/82 , C07D209/88 , C07D225/08 , C07D403/06 , C07D403/14 , C07K1/04 , C07K7/08 , C07K7/56 , G01N33/68 , G06F19/16 , G06F19/18 , C12Q1/00 , A61K38/04 , C07K5/00 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/567
CPC分类号： C07D403/06 , C07D209/82 , C07D209/88 , C07D225/08 , C07D403/14 , C07K1/047 , C07K7/08 , C07K7/56 , C07K2299/00 , C40B40/00 , G01N33/6875 , G06F19/16 , G06F19/18
摘要： The present invention relates to methods and agonist/antagonist compounds for modulating nuclear receptor coactivator binding. The invention includes a method for identifying residues comprising a coactivator binding site for a nuclear receptor of interest. Also included is a method of identifying agonists and/or antagonists that bind to a coactivator binding site of a nuclear receptor of interest. Agonists and antagonists of coactivator binding to nuclear receptors also are provided. The invention is exemplified by identification and manipulation of the coactivator binding site of the thyroid receptor (TR), and compounds that bind to this sites. The methods can be applied to other nuclear receptors including RAR, RXR, PPAR, VDR, ER, GR, PR, MR, and AR.
摘要翻译：本发明涉及用于调节核受体共激活因子结合的方法和激动剂/拮抗剂化合物。本发明包括用于鉴定残留物的方法，所述残基包含感兴趣的核受体的共激活子结合位点。还包括鉴定结合感兴趣的核受体的共激活子结合位点的激动剂和/或拮抗剂的方法。共激活剂与核受体结合的激动剂和拮抗剂也被提供。本发明通过甲状腺受体（TR）的共激活因子结合位点的鉴定和操作以及与该位点结合的化合物来举例说明。该方法可应用于其他核受体，包括RAR，RXR，PPAR，VDR，ER，GR，PR，MR和AR。

6. 发明申请

WO9721993A3 NUCLEAR RECEPTOR LIGANDS AND LIGAND BINDING DOMAINS 审中-公开
标题翻译：核受体配偶和配偶绑定域
公开(公告)号：WO9721993A3
公开(公告)日：1997-07-24
申请号：PCT/US9620778
申请日：1996-12-13
申请人： UNIV CALIFORNIA
发明人： SCANLAN THOMAS S , BAXTER JOHN D , FLETTERICK ROBERT J , WAGNER RICHARD L , KUSHNER PETER J , APRILETTI JAMES L , WEST BRIAN L , SHIAU ANDREW K
IPC分类号： A61K45/00 , A61K31/00 , A61K31/19 , A61K31/192 , A61K31/195 , A61P3/00 , A61P3/06 , A61P5/00 , A61P5/14 , C07K1/00 , C07K14/47 , C07K14/72 , G01N33/48 , G01N33/483 , G01N33/68 , G06F17/50 , G01N
CPC分类号： C07K14/72 , C07K2299/00
摘要： The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three-dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as 'TR'). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.

7. 发明专利

AU763452B2 Nuclear receptor ligands and ligand binding domains 未知
公开(公告)号：AU763452B2
公开(公告)日：2003-07-24
申请号：AU1799999
申请日：1998-11-25
申请人： UNIV CALIFORNIA
发明人： SCANLAN THOMAS S , BAXTER JOHN D , FLETTERICK ROBERT J , WAGNER RICHARD L , KUSHNER PETER J , APRILETTI JAMES W , WEST BRIAN L , SHIAU ANDREW K
IPC分类号： G01N33/50 , A61K31/192 , A61K31/196 , A61K31/198 , A61K31/27 , A61P43/00 , C07K1/00 , C07K14/00 , C07K14/72 , G01N33/15 , G01N33/78 , G06F19/16
摘要： The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as "TR"). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.

8. 发明专利

BR9815061A 未知
公开(公告)号：BR9815061A
公开(公告)日：2001-11-20
申请号：BR9815061
申请日：1998-11-25
申请人： UNIV CALIFORNIA
发明人： SCANLAN THOMAS S , BAXTER JOHN D , FLETTERICK ROBERT J , WAGNER RICHARD L , KUSHNER PETER J , APRILETTI JAMES W , WESTFIELD BRIAN L , SHIAU ANDREW K
IPC分类号： G01N33/50 , A61K31/192 , A61K31/196 , A61K31/198 , A61K31/27 , A61P43/00 , C07K1/00 , C07K14/00 , C07K14/72 , G01N33/15 , G01N33/78 , G06F19/16
摘要： The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as "TR"). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.

9. 发明专利

AU1799999A Nuclear receptor ligands and ligand binding domains 未知
公开(公告)号：AU1799999A
公开(公告)日：1999-06-15
申请号：AU1799999
申请日：1998-11-25
申请人： UNIV CALIFORNIA
发明人： SCANLAN THOMAS S , BAXTER JOHN D , FLETTERICK ROBERT J , WAGNER RICHARD L , KUSHNER PETER J , APRILETTI JAMES W , WEST BRIAN L , SHIAU ANDREW K
IPC分类号： G01N33/50 , A61K31/192 , A61K31/196 , A61K31/198 , A61K31/27 , A61P43/00 , C07K1/00 , C07K14/00 , C07K14/72 , G01N33/15 , G01N33/78 , G06F19/16
摘要： The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as "TR"). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.

10. 发明专利

AU2003220708B2 Nuclear receptor ligands and ligand binding domains 未知
公开(公告)号：AU2003220708B2
公开(公告)日：2005-10-20
申请号：AU2003220708
申请日：2003-07-10
申请人： UNIV CALIFORNIA
发明人： WEST BRIAN L , KUSHNER PETER J , BAXTER JOHN D , WAGNER RICHARD L , APRILETTI JAMES L , SCANLAN THOMAS S , SHIAU ANDREW K , FLETTERICK ROBERT J
IPC分类号： A61K31/192 , A61K31/195 , A61P7/00 , C03B23/00 , C07C65/24 , C07C229/36 , C07C233/47 , C07C235/74 , C07C271/58 , C07C281/02 , C30B23/00 , A61K031/192 , A61K031/195 , A61P007/00 , C03B023/00 , C07C065/24 , C30B023/00

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