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1. 发明申请

US20050208613A1 Common ligand universal enzyme assay and compositions for use therein 审中-公开
标题翻译：普通配体通用酶测定法及其中使用的组合物
公开(公告)号：US20050208613A1
公开(公告)日：2005-09-22
申请号：US11118016
申请日：2005-04-29
申请人： Yong Qin , Lin Yu , Mark Hansen , Eduard Sergienko , Bonnie Bertolaet , Daniel Sem
发明人： Yong Qin , Lin Yu , Mark Hansen , Eduard Sergienko , Bonnie Bertolaet , Daniel Sem
IPC分类号： C12N9/02 , G01N33/566 , C12Q1/26 , C07H19/207
CPC分类号： C12N9/001 , C12Y103/01026 , G01N33/566 , G01N2333/90209 , G01N2500/02
摘要： The present invention provides compositions containing a common ligand linked to a detectable moiety and provides methods for the preparation of such compositions. The present invention also provides methods for screening candidate ligands for binding to a NAD binding receptor, which include contacting a receptor with a candidate ligand and a composition of the invention followed by evaluation of receptor binding. The screening method of the present invention has broad applicability and can be used to screen large numbers of a wide variety of ligands. The present invention further provides methods for detecting the binding activity of a putative receptor, which include combining the putative receptor with a composition of the invention and evaluating the level of detectable moiety. The invention also provides kits useful for detection of receptors having NAD binding activity and for screening of candidate ligands that bind to a NAD binding receptor.
摘要翻译：本发明提供含有与可检测部分连接的共同配体的组合物，并提供制备这种组合物的方法。本发明还提供了筛选用于结合NAD结合受体的候选配体的方法，其包括使受体与候选配体和本发明的组合物接触，然后评估受体结合。本发明的筛选方法具有广泛的适用性，可用于筛选大量各种配体。本发明还提供了用于检测推定受体的结合活性的方法，其包括将推定的受体与本发明的组合物结合并评估可检测部分的水平。本发明还提供了可用于检测具有NAD结合活性的受体并用于筛选结合NAD结合受体的候选配体的试剂盒。

2. 发明申请

US20050019825A9 Common ligand mimics: pseudothiohydantoins 审中-公开
标题翻译：普通配体模拟物：假硫代乙内酰脲
公开(公告)号：US20050019825A9
公开(公告)日：2005-01-27
申请号：US10099136
申请日：2002-03-15
申请人： Qing Dong , Fabrice Pierre , Hengyuan Lang , Lin Yu , Mark Hansen , Daniel Sem , Maurizio Pellecchia
发明人： Qing Dong , Fabrice Pierre , Hengyuan Lang , Lin Yu , Mark Hansen , Daniel Sem , Maurizio Pellecchia
IPC分类号： C07B61/00 , C07D277/20 , C07D277/38 , C07D417/06 , C07D417/12 , G01N33/53 , C07D417/02 , G01N33/543
CPC分类号： C07D277/20 , C07D417/06 , C07D417/12 , C40B40/00 , G01N2500/00
摘要： The present invention provides common ligand mimics that act as common ligands for a receptor family. The present invention also provides bi-ligands containing these common ligand mimics. Bi-ligands of the invention provide enhanced affinity and/or selectivity of ligand binding to a receptor or receptor family through the synergistic action of the common ligand mimic and specificity ligand that compose the bi-ligand. The present invention also provides combinatorial libraries containing the common ligand mimics and bi-ligands of the invention. Further, the present invention provides methods for manufacturing the common ligand mimics and bi-ligands of the invention and methods for assaying the combinatorial libraries of the invention.
摘要翻译：本发明提供了作为受体家族的共同配体的常见配体模拟物。本发明还提供含有这些共同配体模拟物的双配体。本发明的双配体通过构成双配体的共同配体模拟物和特异性配体的协同作用，提供配体与受体或受体家族结合的增强的亲和力和/或选择性。本发明还提供了包含本发明的共同配体模拟物和双配位体的组合文库。此外，本发明提供了制备本发明的共同配体模拟物和双配位体的方法以及用于测定本发明的组合文库的方法。

3. 发明申请

US20050112716A1 NMR-solve method for rapid identification of bi-ligand drug candidates 有权
标题翻译：用于快速鉴定双配体药物候选物的NMR-解决方法
公开(公告)号：US20050112716A1
公开(公告)日：2005-05-26
申请号：US10884181
申请日：2004-07-02
申请人： Daniel Sem , Maurizio Pellecchia , Anna Tempczyk-Russell
发明人： Daniel Sem , Maurizio Pellecchia , Anna Tempczyk-Russell
IPC分类号： C12Q1/32 , G01N33/53 , G01N33/542 , G01N33/68 , C12Q1/68 , G01N33/48 , G01N33/50 , G06F19/00
CPC分类号： C12Q1/00 , C12Q1/32 , C12Q1/485 , G01N33/53 , G01N33/542 , G01N33/6803 , G01N2500/00 , G01N2500/20 , Y10T436/24
摘要： Methods for rapidly identifying drug candidates that can bind to an enzyme at both a common ligand site and a specificity ligand site, resulting in high affinity binding. The bi-ligand drug candidates are screened from a focused combinatorial library where the specific points of variation on a core structure are optimized. The optimal points of variation are identified by which atoms of a ligand bound to the common ligand site are identified to be proximal to the specificity ligand site. As a result, the atoms proximal to the specificity ligand site can then be used as a point for variation to generate a focused combinatorial library of high affinity drug candidates that can bind to both the common ligand site and the specificity ligand site. Different candidates in the library can then have high affinity for many related enzymes sharing a similar common ligand site.
摘要翻译：用于快速鉴定可以在共同配体位点和特异性配体位点处结合酶的候选药物的方法，导致高亲和力结合。双重配体药物候选物从聚焦的组合文库筛选，其中优化核心结构上的特异性变异点。通过与共同配体位点结合的配体的哪个原子被鉴定为接近特异性配体位点来鉴定最佳的变化点。结果，接近特异性配体位点的原子然后可以用作变异点，以产生可以结合共同配体位点和特异性配体位点的高亲和力药物候选物的聚焦组合文库。然后，文库中的不同候选物可以对共享相似共同配体位点的许多相关酶具有高亲和力。

4. 发明申请

US20060166279A1 Sea-trosy and related methods 审中-公开
标题翻译：海y和相关方法
公开(公告)号：US20060166279A1
公开(公告)日：2006-07-27
申请号：US11320157
申请日：2005-12-27
申请人： Daniel Sem , Maurizio Pellecchia
发明人： Daniel Sem , Maurizio Pellecchia
IPC分类号： G01N33/53
CPC分类号： G01R33/4608 , G01R33/465 , Y10T436/24
摘要： A method for preferentially observing an exposed position (1c) of a macromolecule. A sample is obtained having a macromolecule (1a) with a first proton (1) and a second molecule (2a) with a second proton (2); then applying a magnetic field (4) to the sample and irradiating the sample with a pulse sequence (5) that preferentially demagnetizes protons of the macromolecule (1,3) relative to the second proton (2); allowing the second proton (2) to exchange (6) with an exposed proton (1) of the macromolecule; and detecting the magnetization from the relatively magnetized second proton (2), which is now bound to the exposed position (1c) of the macromolecule. The invention also provides a method for observing a position in the macromolecule that bind a ligand.
摘要翻译：优选观察高分子暴露位置（1c）的方法。获得具有第一质子（1）的大分子（1a）和具有第二质子（2）的第二分子（2a）的样品; 然后对样品施加磁场（4）并用脉冲序列（5）照射样品，所述脉冲序列（5）相对于第二质子（2）优先地消磁高分子（1,3）的质子; 允许第二质子（2）与大分子的暴露的质子（1）交换（6）; 并且检测来自相对磁化的第二质子（2）的磁化，其现在与大分子的暴露位置（1c）结合。本发明还提供了观察结合配体的大分子中的位置的方法。

5. 发明申请

US20070054410A1 Dithio compounds 有权
标题翻译：二硫化合物
公开(公告)号：US20070054410A1
公开(公告)日：2007-03-08
申请号：US11512485
申请日：2006-08-30
申请人： Daniel Sem , Phani Pullela
发明人： Daniel Sem , Phani Pullela
IPC分类号： G01N33/50 , C07D311/82
CPC分类号： C07D311/90 , C07D311/82 , C07D335/12 , C07D335/20 , C07D409/12 , Y10T436/182
摘要： Disclosed herein are dithio compounds that include at least one fluorophore. The compounds additionally may include a different fluorophore or a non-fluorophore. The dithio compounds may be used as reagents for detecting thiol-containing compounds.
摘要翻译：本文公开了包含至少一个荧光团的二硫代化合物。化合物另外可以包括不同的荧光团或非荧光团。二硫化合物可用作检测含硫醇化合物的试剂。

6. 发明申请

US20070054343A1 Use of thiol-reactive reagents for detecting enzyme activity 失效
标题翻译：使用硫醇反应试剂检测酶活性
公开(公告)号：US20070054343A1
公开(公告)日：2007-03-08
申请号：US11512832
申请日：2006-08-30
申请人： Daniel Sem
发明人： Daniel Sem
IPC分类号： C12Q1/48
CPC分类号： C12Q1/485 , Y10T436/143333
摘要： Disclosed are assays useful for detecting enzyme activity. The assays may utilize thiol-reactive reagents. The assays may include reacting a reacting mixture that contains an ATP analog (e.g., ATPβS or GTPβS) to form an ADP analog (e.g., ATPβS or GTPβS).
摘要翻译：公开了用于检测酶活性的测定法。测定法可以利用硫醇反应性试剂。测定可以包括使包含ATP类似物（例如ATPbetaS或GTPbetaS）的反应混合物反应以形成ADP类似物（例如ATPβ或GTPβS）。

7. 发明申请

US20070298439A1 NMR-SOLVE METHOD FOR RAPID IDENTIFICATION OF BI-LIGAND DRUG CANDIDATES 审中-公开
标题翻译：用于快速鉴定双配偶药物候选药物的NMR-溶解方法
公开(公告)号：US20070298439A1
公开(公告)日：2007-12-27
申请号：US11833191
申请日：2007-08-02
申请人： Daniel Sem , Maurizio Pellecchia , Anna Tempczyk-Russell
发明人： Daniel Sem , Maurizio Pellecchia , Anna Tempczyk-Russell
IPC分类号： G01N33/573
CPC分类号： C12Q1/00 , C12Q1/32 , C12Q1/485 , G01N33/53 , G01N33/542 , G01N33/6803 , G01N2500/00 , G01N2500/20 , Y10T436/24
摘要： Methods for rapidly identifying drug candidates that can bind to an enzyme at both a common ligand site and a specificity ligand site, resulting in high affinity binding. The bi-ligand drug candidates are screened from a focused combinatorial library where the specific points of variation on a core structure are optimized. The optimal points of variation are identified by which atoms of a ligand bound to the common ligand site are identified to be proximal to the specificity ligand site. As a result, the atoms proximal to the specificity ligand site can then be used as a point for variation to generate a focused combinatorial library of high affinity drug candidates that can bind to both the common ligand site and the specificity ligand site. Different candidates in the library can then have high affinity for many related enzymes sharing a similar common ligand site.
摘要翻译：用于快速鉴定可以在共同配体位点和特异性配体位点处结合酶的候选药物的方法，导致高亲和力结合。双重配体药物候选物从聚焦的组合文库筛选，其中优化核心结构上的特异性变异点。通过与共同配体位点结合的配体的哪个原子被鉴定为接近特异性配体位点来鉴定最佳的变化点。结果，接近特异性配体位点的原子然后可以用作变异点，以产生可以结合共同配体位点和特异性配体位点的高亲和力药物候选物的聚焦组合文库。然后，文库中的不同候选物可以对共享相似共同配体位点的许多相关酶具有高亲和力。

8. 发明申请

US20050234652A1 Nuclear magnetic resonance-docking of compounds 审中-公开
标题翻译：化合物的核磁共振对接
公开(公告)号：US20050234652A1
公开(公告)日：2005-10-20
申请号：US11115850
申请日：2005-04-26
申请人： Daniel Sem , Maurizio Pellecchia
发明人： Daniel Sem , Maurizio Pellecchia
IPC分类号： G01N24/08 , G01R33/46 , G01R33/465 , G06F19/00 , G01N33/48 , G01N33/50
CPC分类号： G01N24/08 , G01R33/4625 , G01R33/465 , Y10T436/24
摘要： The invention provides a method for determining a structure model for a test ligand bound to a macromolecule binding site. Structural constraints for the test ligand are derived from spectroscopic signals arising from interactions between the test ligand and macromolecule. The structure constraints are used as constraints in docking a structure model of the ligand to a structure model of the macromolecule, or as constraints in overlaying a structure model of the test ligand on the known structure for a reference ligand that binds to the macromolecule. The invention further provides a method for determining a structure model for a macromolecule bound to a ligand. Structural constraints derived from spectroscopically observed interactions of the macromolecule and a reference ligand are used to guide molecular modeling or to evaluate the results of a molecular modeling simulation of the macromolecule.
摘要翻译：本发明提供了一种确定与大分子结合位点结合的测试配体的结构模型的方法。测试配体的结构约束来源于由测试配体和大分子之间的相互作用产生的光谱信号。结构约束被用作将配体的结构模型对接到大分子的结构模型的约束，或作为将测试配体的结构模型重叠在与大分子结合的参考配体的已知结构上的限制。本发明还提供了一种用于测定与配体结合的大分子的结构模型的方法。用大分子和参考配体的光谱观察相互作用衍生的结构约束用于指导分子建模或评估大分子的分子模拟模拟的结果。

9. 发明申请

US20050214868A1 Multi-partite ligands and methods of identifying and using same 审中-公开
标题翻译：多分子配体及其识别和使用方法
公开(公告)号：US20050214868A1
公开(公告)日：2005-09-29
申请号：US11126445
申请日：2005-05-10
申请人： Daniel Sem
发明人： Daniel Sem
IPC分类号： G01N33/50 , A61K51/00 , C07B61/00 , C07G99/00 , C12Q1/00 , C12Q1/02 , C12Q1/25 , G01N33/53 , G01N33/542 , G01N33/566
CPC分类号： G01N33/542 , C12Q1/00 , G01N33/566 , Y02A50/58
摘要： The invention provides methods for generating a library of bi-ligands, comprising (a) determining a common ligand to a conserved site in a receptor family; (b) attaching an expansion linker to the common ligand, wherein the expansion linker has sufficient length and orientation to direct a second ligand to a specificity site of a receptor in the receptor family, to form a module; and (c) generating a population of bi-ligands comprising a plurality of identical modules attached to variable second ligands. The invention also provides methods for identifying a bi-target ligand to a receptor by combining a first bi-ligand to a first receptor in a receptor family and a second bi-ligand to a second receptor in the receptor family. The invention additionally provides bi-ligands and bi-target ligands.
摘要翻译：本发明提供了生成双配体文库的方法，其包括（a）确定受体家族中保守位点的共同配体; （b）将扩增接头连接到共同配体，其中所述扩增接头具有足够的长度和取向以将第二配体引导至受体家族中受体的特异性位点以形成模块; 和（c）产生包含连接到可变第二配体的多个相同模块的双配体群体。本发明还提供了通过将受体家族中的第一双配体与受体家族中的第一受体和第二双配体结合到受体家族中的第二受体来鉴定受体的双靶配体的方法。本发明另外提供双配体和双靶配体。

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