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公开(公告)号：US20050059135A1
公开(公告)日：2005-03-17
申请号：US10752478
申请日：2004-01-05
Applicant: Christine Klein , Andrew Murphy , Dana Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
Inventor： Christine Klein , Andrew Murphy , Dana Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
IPC: C07K14/395 , C12N5/02 , C12N15/81 , C07H21/04 , C07K14/705 , C12N1/18
CPC classification number: C12N15/81 , C07K14/395 , C07K2319/02
Abstract: The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assay enables rapid screening of large numbers of polypeptides in a library to identifying those polypeptides which induce or antagonize receptor bioactivity. The subject assay is particularly amenable for identifying surrogate ligands for orphan receptors.
Abstract translation: 本发明提供用于筛选和鉴定与细胞受体或离子通道的活性特异性相互作用并调节其活性的药学有效化合物的快速有效的测定。 本发明分析使得能够快速筛选文库中的大量多肽以鉴定诱导或拮抗受体生物活性的那些多肽。 主题测定特别适用于鉴定孤儿受体的替代配体。
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公开(公告)号：US07250263B2
公开(公告)日：2007-07-31
申请号：US10752478
申请日：2004-01-05
Applicant: Christine A. Klein , Andrew J. M. Murphy , Dana M. Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
Inventor： Christine A. Klein , Andrew J. M. Murphy , Dana M. Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
CPC classification number: C12N15/81 , C07K14/395 , C07K2319/02
Abstract: The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assay enables rapid screening of large numbers of polypeptides in a library to identifying those polypeptides which induce or antagonize receptor bioactivity. The subject assay is particularly amenable for identifying surrogate ligands for orphan receptors.
Abstract translation: 本发明提供用于筛选和鉴定与细胞受体或离子通道的活性特异性相互作用并调节其活性的药学有效化合物的快速有效的测定。 本发明分析使得能够快速筛选文库中的大量多肽以鉴定诱导或拮抗受体生物活性的那些多肽。 主题测定特别适用于鉴定孤儿受体的替代配体。
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Patent Agency Ranking
公开(公告)号：US20070154947A1
公开(公告)日：2007-07-05
申请号：US11513594
申请日：2006-08-31
Applicant: James Broach , Addison Ault
Inventor： James Broach , Addison Ault
IPC: G01N33/53 , G01N33/569 , C07K16/28
CPC classification number: G01N33/54386 , B01J2219/00725 , B01J2219/00743 , G01N33/566 , G01N2333/726
Abstract: In one embodiment the invention provides a mutant UDP-glucose receptor (P2Y14) functionally expressed in the yeast Saccharomyces. The mutant receptors have ligand-binding properties that are useful as practical biosensors. Mutagenesis of the entire UDP-glucose receptor gene yielded receptors with increased activity but similar ligand specificities, while random mutagenesis of residues in the immediate vicinity of the ligand-binding pocket yielded mutants with altered ligand specificity. The receptor mutants can be used to detect chemical ligands in complex mixtures and to discriminate among chemically or stereochemically related compounds. Also provided are methods for combinatorial applications wherein engineered receptors can be applied, for example, in a pairwise manner to differentiate among several chemical analytes that would be indistinguishable with a single receptor.
Abstract translation: 在一个实施方案中，本发明提供了在酵母酵母中功能性表达的突变UDP-葡萄糖受体（P2Y14）。 突变体受体具有可用作实际生物传感器的配体结合特性。 整个UDP-葡萄糖受体基因的诱变产生具有增加的活性但相似的配体特异性的受体，而在配体结合口袋附近随机诱变残基产生具有改变的配体特异性的突变体。 受体突变体可用于检测复杂混合物中的化学配体，并区分化学或立体化学相关化合物。 还提供了用于组合应用的方法，其中工程化受体可以例如以成对方式应用于区分几种与单一受体无法区分的化学分析物。
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公开(公告)号：US07122305B2
公开(公告)日：2006-10-17
申请号：US09747774
申请日：2000-12-21
Applicant: Christine A. Klein , Andrew J. Murphy , Dana M. Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
Inventor： Christine A. Klein , Andrew J. Murphy , Dana M. Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
CPC classification number: C12N15/81 , C07K14/395 , C07K2319/02
Abstract: The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assay enables rapid screening of large numbers of polypeptides in a library to identifying those polypeptides which induce or antagonize receptor bioactivity. The subject assay is particularly amenable for identifying surrogate ligands for orphan receptors.
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5.发明申请公开(公告)号：US20050202403A1
公开(公告)日：2005-09-15
申请号：US10967087
申请日：2004-10-15
Applicant: Dana Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart , Christine Klein , Andrew Murphy
Inventor： Dana Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart , Christine Klein , Andrew Murphy
CPC classification number: G01N33/50 , C07K14/395 , C07K14/4722 , C07K14/705 , C07K14/723 , C07K2319/00 , C07K2319/02 , C12N1/16 , C12N15/81 , C40B30/06 , G01N33/566 , G01N2333/726 , G01N2500/02
Abstract: The present invention pertains to novel yeast cells which are useful for the expression of heterologous G protein coupled receptors. The yeast cells of the present invention can be used in screening assays which can be used to screen for modulators of G protein coupled receptors. Specifically, the invention provides novel yeast cells which express a heterologous G protein coupled receptor and mutant and/or chimeric G protein subunit molecules which serve to functionally integrate the heterologous into the pheromone signaling pathway of the yeast cell. The invention also provides for the expression of heterologous G protein coupled receptors which are functionally integrated into the yeast cell membrane using a yeast a factor leader sequence. Drug discovery assays using the subject yeast cells are also provided.
Abstract translation: 本发明涉及可用于表达异源G蛋白偶联受体的新型酵母细胞。 本发明的酵母细胞可用于筛选测定，其可用于筛选G蛋白偶联受体的调节剂。 具体地，本发明提供了表达异源G蛋白偶联受体和突变体和/或嵌合G蛋白亚基分子的新型酵母细胞，其用于将异源整合到酵母细胞的信息素信号通路中。 本发明还提供异源G蛋白偶联受体的表达，其使用酵母因子前导序列在功能上整合到酵母细胞膜中。 还提供使用本发明酵母细胞的药物发现测定。
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公开(公告)号：US06255059B1
公开(公告)日：2001-07-03
申请号：US08582333
申请日：1996-01-17
Applicant: Christine A. Klein , Andrew J. M. Murphy , Dana M. Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
Inventor： Christine A. Klein , Andrew J. M. Murphy , Dana M. Fowlkes , James Broach , John Manfredi , Jeremy Paul , Joshua Trueheart
IPC: C12N510
CPC classification number: C12N15/81 , C07K14/395 , C07K2319/02
Abstract: The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assay enables rapid screening of large numbers of polypeptides in a yeast expression library to identifying those polypeptides which induce or antagonize receptor bioactivity. The subject assay is particularly amenable for identifying surrogate ligands for orphan receptors.
Abstract translation: 本发明提供用于筛选和鉴定与细胞受体或离子通道的活性特异性相互作用并调节其活性的药学有效化合物的快速有效的测定。 本发明分析使得能够在酵母表达文库中快速筛选大量多肽，以鉴定诱导或拮抗受体生物活性的那些多肽。 主题测定特别适用于鉴定孤儿受体的替代配体。
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公开(公告)号：US20080070794A1
公开(公告)日：2008-03-20
申请号：US11804905
申请日：2007-05-21
Applicant: James Broach , Addison Ault , Ho Fung , Christodoulos Floudas
Inventor： James Broach , Addison Ault , Ho Fung , Christodoulos Floudas
CPC classification number: G01N33/54386 , B01J2219/00725 , B01J2219/00743 , G01N33/566 , G01N2333/726
Abstract: In one embodiment the invention provides a mutant UDP-glucose receptor (P2Y14) functionally expressed in the yeast Saccharomyces. The mutant receptors have ligand-binding properties that are useful as practical biosensors. Mutagenesis of the entire UDP-glucose receptor gene yielded receptors with increased activity but similar ligand specificities, while random mutagenesis of residues in the immediate vicinity of the ligand-binding pocket yielded mutants with altered ligand specificity. The receptor mutants can be used to detect chemical ligands in complex mixtures and to discriminate among chemically or stereochemically related compounds. Also provided are methods for combinatorial applications wherein engineered receptors can be applied, for example, in a pairwise manner to differentiate among several chemical analytes that would be indistinguishable with a single receptor.
Abstract translation: 在一个实施方案中，本发明提供了在酵母酵母中功能性表达的突变UDP-葡萄糖受体（P2Y14）。 突变体受体具有可用作实际生物传感器的配体结合特性。 整个UDP-葡萄糖受体基因的诱变产生具有增加的活性但相似的配体特异性的受体，而在配体结合口袋附近随机诱变残基产生具有改变的配体特异性的突变体。 受体突变体可用于检测复杂混合物中的化学配体，并区分化学或立体化学相关化合物。 还提供了用于组合应用的方法，其中工程化受体可以例如以成对方式应用于区分几种与单一受体无法区分的化学分析物。
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