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1. 发明授权

US07869958B2 Structure-based modulators of B1 G-protein coupled receptors 有权
标题翻译： B1 G蛋白偶联受体的基于结构的调节剂
公开(公告)号：US07869958B2
公开(公告)日：2011-01-11
申请号：US11199821
申请日：2005-08-09
申请人： Grace Christy Rani Royappa , Marilyn H. Perrin , Jean E. Rivier , Wylie W. Vale, Jr. , Roland Riek
发明人： Grace Christy Rani Royappa , Marilyn H. Perrin , Jean E. Rivier , Wylie W. Vale, Jr. , Roland Riek
IPC分类号： G06G7/58
CPC分类号： C07K14/723 , C07K2299/00 , G01N2333/726 , G06F19/16 , G06F19/18
摘要： The present invention relates to a method for identifying modulators of B1 G-protein coupled receptors. The present invention also relates to a method for identifying an antagonist or agonist of the corticotropin-releasing factor receptor 2 (CRFR2). The present invention also relates to a method for improving antagonists or agonists of CRFR2. The present invention also relates to the three-dimensional structure of CRFR2 as representative of the B1 GPCR subfamily and its use as a basis for rational drug design of antagonist or agonists of B1 GPCRs.
摘要翻译：本发明涉及用于鉴定B1G-蛋白偶联受体调节剂的方法。本发明还涉及用于鉴定促肾上腺皮质激素释放因子受体2（CRFR2）的拮抗剂或激动剂的方法。本发明还涉及一种改善CRFR2拮抗剂或激动剂的方法。本发明还涉及作为B1GPCR亚族的代表性的CRFR2的三维结构及其作为B1GPCR的拮抗剂或激动剂的合理药物设计的基础的用途。

2. 发明申请

US20100036096A1 COMPOSITIONS AND METHODS FOR PRODUCING RECOMBINANT PROTEINS 失效
标题翻译：用于生产重组蛋白的组合物和方法
公开(公告)号：US20100036096A1
公开(公告)日：2010-02-11
申请号：US12540852
申请日：2009-08-13
申请人： Tarmo Roosild , Jason Greenwald , Senyon Choe , Roland Riek
发明人： Tarmo Roosild , Jason Greenwald , Senyon Choe , Roland Riek
IPC分类号： C07K14/00 , C07H21/04 , C12N15/63 , C12N5/10 , C12P21/06
CPC分类号： C07K14/32 , C07K2319/01 , C07K2319/03
摘要： A class of integral membrane proteins, referred to as Mistic polypeptides, their variants, fusion proteins including a Mistic polypeptide domain, and nucleic acid molecules encoding Mistic polypeptides and Mistic fusion proteins are disclosed herein. Also described are methods of using Mistic polypeptides and Mistic fusion proteins to produce and/or isolate recombinant proteins (including without limitation classes of eukaryotic proteins that have previously been intractable to recombinant bacterial expression, such as, eukaryotic integral membrane proteins).
摘要翻译：本文公开了一类称为Mistic多肽，其变体，融合蛋白（包括Mistic多肽结构域）和编码Mistic多肽和Mistic融合蛋白的核酸分子的整合膜蛋白。还描述了使用Mistic多肽和Mistic融合蛋白来产生和/或分离重组蛋白（包括但不限于以前对重组细菌表达难以处理的真核蛋白的类别，例如真核整合膜蛋白）的方法。

3. 发明授权

US07612186B2 Compositions and methods for producing recombinant proteins 失效
标题翻译：用于生产重组蛋白的组合物和方法
公开(公告)号：US07612186B2
公开(公告)日：2009-11-03
申请号：US11317847
申请日：2005-12-22
申请人： Tarmo Roosild , Jason Greenwald , Senyon Choe , Roland Riek
发明人： Tarmo Roosild , Jason Greenwald , Senyon Choe , Roland Riek
IPC分类号： C07H21/00 , C12N1/21 , C07K17/02
CPC分类号： C07K14/32 , C07K2319/01 , C07K2319/03
摘要： A class of integral membrane proteins, referred to as Mistic polypeptides, their variants, fusion proteins including a Mistic polypeptide domain, and nucleic acid molecules encoding Mistic polypeptides and Mistic fusion proteins are disclosed herein. Also described are methods of using Mistic polypeptides and Mistic fusion proteins to produce and/or isolate recombinant proteins (including without limitation classes of eukaryotic proteins that have previously been intractable to recombinant bacterial expression, such as, eukaryotic integral membrane proteins).
摘要翻译：本文公开了一类称为Mistic多肽，其变体，融合蛋白（包括Mistic多肽结构域）和编码Mistic多肽和Mistic融合蛋白的核酸分子的整合膜蛋白。还描述了使用Mistic多肽和Mistic融合蛋白来产生和/或分离重组蛋白（包括但不限于以前对重组细菌表达难以处理的真核蛋白的类别，例如真核整合膜蛋白）的方法。

4. 发明申请

US20050245438A1 Receptor(SSTR4)-selective somatostatin analogs 有权
标题翻译：受体（SSTR4） - 选择性生长抑素类似物
公开(公告)号：US20050245438A1
公开(公告)日：2005-11-03
申请号：US11041676
申请日：2005-01-24
申请人： Jean Rivier , Jean Reubi , Judit Erchegyi , Roland Riek
发明人： Jean Rivier , Jean Reubi , Judit Erchegyi , Roland Riek
IPC分类号： A61K38/00 , A61K38/12 , C07K14/655
CPC分类号： C07K14/655 , A61K38/00
摘要： Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,CβMe-L-2Nal8]-SRIF, and counterparts incorporating D-Cys3 and/or D-Trp8 and/or Ala11, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.
摘要翻译：与其他克隆的SRIF受体相比，选择性SSTR4的SRIF的类似物可用于确定受体SSTR4的组织和细胞表达及其在调节肿瘤生长中的生物学作用。 SRIF类似物肽，例如des-AA 1,2,4,5,12,13，[Ala 7] -SRIF; des-AA 1,2,4,5,12,13 [Aph7] -SRIF，des-AA 1,2,4,5,12 ，13β-Cpm-SRIF; des-AA 1,2,4,5,12,13 [Tyr2]，Ala7-Cbm-SRIF，和des- AA 1,2,4,5,12,13 [Tyr 7]，C 2 H 2 Me-L-2Nal 8， SUP]] - SRIF，以及掺有D-Cys 3和/或D-Trp 8和/或Ala 11的对应物与高结合对克隆的人受体SSTR4的亲和力并激活受体，但它们不以与人SSTR1，SSTR2，SSTR3或SSTR5的显着亲和力结合。通过在这些SSTR4选择性SRIF类似物中加入位置2的碘化酪氨酸，可以提供用于药物筛选方法的标记化合物。或者，为了用于治疗，细胞毒素或高度放射性元素可以是N-末端偶联或与其复合的。

5. 发明授权

US06396267B1 Polarization transfer by cross-correlated relaxation in solution NMR with very large molecules 有权
标题翻译：在具有非常大分子的溶液NMR中通过交叉相关松弛的极化转移
公开(公告)号：US06396267B1
公开(公告)日：2002-05-28
申请号：US09487929
申请日：2000-01-19
申请人： Roland Riek , Gerhard Wider , Konstantin Pervushin , Kurt Wuethrich
发明人： Roland Riek , Gerhard Wider , Konstantin Pervushin , Kurt Wuethrich
IPC分类号： G01V300
CPC分类号： G01R33/4608
摘要： A method for performing polarization transfer in NMR experiments with coupled spin ½ nuclei I and S being irradiated by a sequence of rf pulses comprising a first 90° pulse exciting the spins of the nuclei I and after a delay time a further 90° pulse exciting the spins of the nuclei S is characterized in that there is no inversion pulse acting on the spins of the nuclei S during a time period T between the first 90° pulse exciting the spins of the nuclei I and either the further 90° pulse exciting the spins of the nuclei S or a second 90° pulse acting on the spins of the nuclei I, and that the length of the time period T is chosen such that d/dT[{square root over (sinh+L (RCT+L )2+L +sin(&pgr;JIST+L )2+L )} exp(−RIT)] is minimized, where RC is the transverse cross-correlation-relaxation rate of nuclei I, RI is the total transverse relaxation rate of nuclei I and JIS is the scalar coupling constant between nuclei I and S. This provides a novel polarization transfer element which can be used as a “building block” for a great variety of complex NMR experiments including macromolecules with molecular weights far beyond 100000 and yielding higher sensitivity in comparison with methods according to the state of the art such as INEPT.
摘要翻译：在NMR实验中进行极化转移的方法，其中耦合的自旋½核I和S被包括激发核I的自旋的第一90°脉冲的rf脉冲序列照射，并且在延迟时间之后进一步90°脉冲激发核S的自旋特征在于，在激发核I的自旋的第一90°脉冲和激励自旋的另外的90°脉冲之间的时间段T期间，没有反作用脉冲作用在核S的自旋上的核S或作用在核I的自旋上的第二90°脉冲，并且选择时间段T的长度，使得最小化，其中，C i是核I的横向互相关松弛率，RI是核I和JIS的总横向松弛率是核I和S之间的标量耦合常数。这提供了一种新型的极化转移元件，其可以用作各种复杂NMR实验的“构建块”，包括分子量远远超过100000的uding大分子，与根据现有技术的方法如INEPT相比，产生更高的灵敏度。

6. 发明授权

US6133736A Transverse relaxation-optimized spectroscopy (=TROSY) 有权
标题翻译：横向弛豫优化光谱（= TROSY）
公开(公告)号：US6133736A
公开(公告)日：2000-10-17
申请号：US164278
申请日：1998-10-01
申请人： Konstantin Pervushin , Gerhard Wider , Roland Riek , Kurt Wuthrich
发明人： Konstantin Pervushin , Gerhard Wider , Roland Riek , Kurt Wuthrich
IPC分类号： G01N24/08 , A61K49/06 , G01R33/46 , G01R33/465 , G01V3/00
CPC分类号： G01R33/4608 , A61K49/06
摘要： A method for obtaining a nuclear magnetic resonance (NMR) correlation spectrum of heteronuclear spin systems, in particular comprising large molecules, especially biological macromolecules in solution, the spin system being subjected to a homogeneous magnetic field B.sub.0, being irradiated by a sequence of radio frequency (rf) pulses, is characterized in that the spin system comprises at least two kinds of spin 1/2 nuclei I and S being coupled to each other, whereby the sequence of rf pulses is chosen such that line broadening in the observed spectrum due to transverse relaxation (T.sub.2) is significantly reduced because of cross correlation between dipole--dipole (DD) coupling of the spins and chemical shift anisotropy (CSA), giving rise to different relaxation rates of the individual multiplet components of the spin system and chosen such that the relaxation effects of the two different mechanisms cancel each other out to a large degree. Thus, even very large biological macromolecules can be measured.
摘要翻译：一种获得异核自旋体系的核磁共振（NMR）相关谱的方法，特别是包括大分子，尤其是溶液中的生物大分子，旋转系统受到均匀磁场B0的照射，由射频序列（rf）脉冲的特征在于，自旋系统包括至少两种旋转+ E，fra 1/2 + EE核I和S彼此耦合，由此选择rf脉冲序列使得线展宽由于横向松弛（T2）的观察光谱由于自旋的偶极 - 偶极（DD）耦合和化学位移各向异性（CSA）之间的相互关系而显着降低，导致了各种多重态分量的松弛率不同旋转系统并选择使得两种不同机制的松弛效果在很大程度上相互抵消。因此，甚至可以测量非常大的生物大分子。

7. 发明申请

US20060069516A1 Structure-based modulators of B1 G-protein coupled receptors 有权
标题翻译： B1 G蛋白偶联受体的基于结构的调节剂
公开(公告)号：US20060069516A1
公开(公告)日：2006-03-30
申请号：US11199821
申请日：2005-08-09
申请人： Grace Royappa , Marilyn Perrin , Jean Rivier , Wylie Vale , Roland Riek
发明人： Grace Royappa , Marilyn Perrin , Jean Rivier , Wylie Vale , Roland Riek
IPC分类号： G06F19/00
CPC分类号： C07K14/723 , C07K2299/00 , G01N2333/726 , G06F19/16 , G06F19/18
摘要： The present invention relates to a method for identifying modulators of B1 G-protein coupled receptors. The present invention also relates to a method for identifying an antagonist or agonist of the corticotropin-releasing factor receptor 2 (CRFR2). The present invention also relates to a method for improving antagonists or agonists of CRFR2. The present invention also relates to the three-dimensional structure of CRFR2 as representative of the B1 GPCR subfamily and its use as a basis for rational drug design of antagonist or agonists of B1 GPCRs.
摘要翻译：本发明涉及用于鉴定B1G-蛋白偶联受体调节剂的方法。本发明还涉及用于鉴定促肾上腺皮质激素释放因子受体2（CRFR2）的拮抗剂或激动剂的方法。本发明还涉及一种改善CRFR2拮抗剂或激动剂的方法。本发明还涉及作为B1GPCR亚族的代表性的CRFR2的三维结构及其作为B1GPCR的拮抗剂或激动剂的合理药物设计的基础的用途。

8. 发明授权

US07238775B2 Receptor(SSTR4)-selective somatostatin analogs 有权
标题翻译：受体（SSTR4） - 选择性生长抑素类似物
公开(公告)号：US07238775B2
公开(公告)日：2007-07-03
申请号：US11041676
申请日：2005-01-24
申请人： Jean E. F. Rivier , Jean Claude Reubi , Judit Erchegyi , Roland Riek
发明人： Jean E. F. Rivier , Jean Claude Reubi , Judit Erchegyi , Roland Riek
IPC分类号： A61K38/00
CPC分类号： C07K14/655 , A61K38/00
摘要： Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,CβMe-L-2Nal8]-SRIF, and counterparts incorporating D-Cys3 and/or D-Trp8 and/or Ala11, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.
摘要翻译：与其他克隆的SRIF受体相比，选择性SSTR4的SRIF的类似物可用于确定受体SSTR4的组织和细胞表达及其在调节肿瘤生长中的生物学作用。 SRIF类似物肽，例如des-AA 1,2,4,5,12,13，[Ala 7] -SRIF; des-AA 1,2,4,5,12,13 [Aph7] -SRIF，des-AA 1,2,4,5,12 ，13β-Cpm-SRIF; des-AA 1,2,4,5,12,13 [Tyr2]，Ala7-Cbm-SRIF，和des- AA 1,2,4,5,12,13 [Tyr 7]，C 2 H 2 Me-L-2Nal 8， SUP]] - SRIF，以及掺有D-Cys 3和/或D-Trp 8和/或Ala 11的对应物与高结合对克隆的人受体SSTR4的亲和力并激活受体，但它们不以与人SSTR1，SSTR2，SSTR3或SSTR5的显着亲和力结合。通过在这些SSTR4选择性SRIF类似物中加入位置2的碘化酪氨酸，可以提供用于药物筛选方法的标记化合物。或者，为了用于治疗，细胞毒素或高度放射性元素可以是N-末端偶联或与其复合的。

9. 发明申请

US20060211087A1 Compositions and methods for producing recombinant proteins 失效
公开(公告)号：US20060211087A1
公开(公告)日：2006-09-21
申请号：US11317847
申请日：2005-12-22
申请人： Tarmo Roosild , Jason Greenwald , Senyon Choe , Roland Riek , Mark Vega
发明人： Tarmo Roosild , Jason Greenwald , Senyon Choe , Roland Riek , Mark Vega
IPC分类号： C07K14/705 , C07H21/04 , C12P21/06
CPC分类号： C07K14/32 , C07K2319/01 , C07K2319/03
摘要： A class of integral membrane proteins, referred to as Mistic polypeptides, their variants, fusion proteins including a Mistic polypeptide domain, and nucleic acid molecules encoding Mistic polypeptides and Mistic fusion proteins are disclosed herein. Also described are methods of using Mistic polypeptides and Mistic fusion proteins to produce and/or isolate recombinant proteins (including without limitation classes of eukaryotic proteins that have previously been intractable to recombinant bacterial expression, such as, eukaryotic integral membrane proteins).

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