-
41.发明授权公开(公告)号：US07807140B2
公开(公告)日：2010-10-05
申请号：US11743740
申请日：2007-05-03
IPC分类号： A61B5/055
CPC分类号： A61K49/128
摘要： Polymeric chelating agents and metal chelates, particularly those of lanthanide metals and more specifically those of Gd(III), useful as contrast agents in magnetic resonance imaging (MRI) for therapeutic and diagnostic applications as well as clinical and biomedical research applications. The polymeric chelates are generated using ring-opening metathesis polymerization (ROMP). Polymers can have multiple sites for functionalization allowing for the synthesis of multimodal and targeted contrast agents. Hydroxypyridonate (HOPO)-based chelating moieties are integrated into a ROMP-derived polymer. More specifically, the HOPO-based chelating moiety is integrated into a benzonorbornadiene unit that constitutes the backbone of the polymer. The ROMP-derived polymer chelators can comprise multiple metal ions, particularly Gd(III) ions, in polymers of varying lengths to provide a series of agents with controlled relaxivites. Polymer chelates include those that are water-soluble.
摘要翻译： 聚合螯合剂和金属螯合物，特别是镧系元素金属螯合剂，更具体地，可用作Gd（III）的螯合剂，用作治疗和诊断应用以及临床和生物医学研究应用的磁共振成像（MRI）中的造影剂。 使用开环易位聚合（ROMP）产生聚合物螯合物。 聚合物可以具有多个用于官能化的位点，允许合成多峰和靶向造影剂。 将羟基吡啶酮（HOPO）基螯合部分整合到ROMP衍生的聚合物中。 更具体地，基于HOPO的螯合部分整合成构成聚合物主链的苯并降二烯单元。 ROMP衍生的聚合物螯合剂可以在不同长度的聚合物中包含多种金属离子，特别是Gd（III）离子，以提供具有受控弛豫物质的一系列试剂。 聚合物螯合物包括那些水溶性螯合物。
-
公开(公告)号：US06914048B2
公开(公告)日：2005-07-05
申请号：US10246441
申请日：2002-09-18
CPC分类号： C07K7/08 , A61K47/645 , C07K7/06
摘要： Disclosed are β-peptides and β-peptide conjugates that are capable of diffusing or otherwise being transported across the cell membranes of living cells. The β-peptides contain at least six β-amino acid residues, at leastsix of which are preferably β3-homoarginine residues. It has been found that when pharmacologically-active agents are conjugated to these types of β-peptides, the resulting conjugates (also disclosed herein) are also capable of diffusing or otherwise being transported across the cell membranes of living cells, including mammalian cells.
摘要翻译： 公开了能够扩散或以其它方式被传输通过活细胞细胞膜的β-肽和β-肽缀合物。 β-肽含有至少六个β-氨基酸残基，其中至少有七个是优质β-OH-精氨酸残基。 已经发现，当药理活性剂与这些类型的β-肽缀合时，所得到的缀合物（本文也公开）也能够扩散或以其它方式被传输穿过包括哺乳动物细胞的活细胞的细胞膜。
-
公开(公告)号：US06833489B1
公开(公告)日：2004-12-21
申请号：US09663805
申请日：2000-09-15
IPC分类号： G01N3300
CPC分类号： A01K67/0336 , A01K2217/058 , A01K2217/075 , A01K2227/703 , A01K2267/03 , C12N9/0069 , C12N15/8509 , G01N33/5085 , G01N2333/43534 , G01N2333/90245
摘要： A method for evaluating a test compound's ability to modulate prolyl 4-hydroxylase is disclosed. In one embodiment, the method comprises the steps of introducing a test compound into a test chimeric, P4H-gene modified, or a wild-type nematode, wherein the test chimeric nematode has a complemented prolyl-4-hydroxylase gene mutation, and observing the effect of the test compound on the prolyl 4-hydroxylase activity of the progeny of the test chimeric, P4H-gene modified, or the wild-type nematode, wherein a dpy or embryonic lethal phenotype indicates prolyl-4-hydroxylase inhibition.
摘要翻译： 公开了一种用于评估测试化合物调节脯氨酰4-羟化酶的能力的方法。 在一个实施方案中，该方法包括以下步骤：将测试化合物引入测试嵌合，P4H基因修饰或野生型线虫中，其中测试嵌合线虫具有互补的脯氨酰-4-羟化酶基因突变，并观察 测试化合物对测试嵌合体，P4H-基因修饰的或野生型线虫的后代的脯氨酰4-羟化酶活性的影响，其中dpy或胚胎致死表型表示脯氨酰-4-羟化酶抑制。
-
公开(公告)号：US5973112A
公开(公告)日：1999-10-26
申请号：US918223
申请日：1997-08-25
申请人： Ronald T. Raines
发明人： Ronald T. Raines
摘要： A novel collagen mimic comprising a tripeptide unit having the formula (XaaFlpGly).sub.n, where Flp is 4(R)-fluoro-L-proline, is disclosed. The collagen mimic has increased stability relative to the collagen-related triple helices (ProProGly).sub.n and (ProHypGly).sub.n.
摘要翻译： 公开了包含具有式（XaaFlpGly）n的三肽单元的新型胶原模拟物，其中Flp是4（R） - 氟-L-脯氨酸。 胶原模拟物相对于胶原相关的三重螺旋（ProProGly）n和（ProHypGly）n具有增加的稳定性。
-
公开(公告)号：US5817455A
公开(公告)日：1998-10-06
申请号：US639806
申请日：1996-04-29
申请人： Ronald T. Raines
发明人： Ronald T. Raines
CPC分类号： C12Q1/44 , G01N2333/922
摘要： A method for inactivating, at a desired stage of an in vitro process, a target enzyme having coupled thereto a biotin molecule, includes adding to a reaction mix an inactivating protein having an affinity for the biotin molecule that is sufficient to inhibit the activity of the target enzyme. The method is embodied in the ribonuclease activity of the enzyme RNase S, which can be active in a form composed of an S peptide and an S protein, not covalently bound together, which associate to form the catalytic molecule. By adding an affinity moeity to the S peptide, it is possible to a second, inactivating protein having affinity for the affinity moeity to disassociate the S peptide from the S protein, and thereby terminate catalytic activity of RNase S at a desired point in any reaction.
摘要翻译： 一种用于在体外过程的期望阶段使与其偶联的生物素分子的靶酶失活的方法包括向反应混合物中加入对生物素分子具有亲和力的灭活蛋白，其足以抑制生物素活性 靶酶。 该方法体现在酶RNase S的核糖核酸酶活性中，其可以以不共价结合在一起形成催化分子的由S肽和S蛋白组成的形式活性。 通过向S肽添加亲和力，可以使具有亲和力的亲和力的第二失活蛋白从S蛋白脱离S肽，从而终止任何反应中所需点的RNase S的催化活性 。
-
公开(公告)号：US5389537A
公开(公告)日：1995-02-14
申请号：US184604
申请日：1994-01-21
IPC分类号： C12N9/22
CPC分类号： C12N9/22 , Y10S435/81
摘要： A ribonuclease molecule altered at a single amino acid, relative to its wild-type form, displays altered substrate specificity and substrate binding mechanism. The altered protein cleaves RNA efficiently after C, U and A residues, whereas the wild-type protein cannot cleave efficiently after A. The change that alters the specificity also permits the protein to cleave poly (A) portions of an RNA molecule processively.
摘要翻译： 相对于其野生型形式，在单个氨基酸处改变的核糖核酸酶分子显示改变的底物特异性和底物结合机制。 改变的蛋白质在C，U和A残基之后有效地切割RNA，而野生型蛋白质在A后不能有效切割。改变特异性的变化也允许蛋白质切割RNA分子的聚（A）部分。
-
公开(公告)号：US20130196433A1
公开(公告)日：2013-08-01
申请号：US13745737
申请日：2013-01-18
申请人： Ronald T. Raines , Gregory Ellis , Michael Palte
发明人： Ronald T. Raines , Gregory Ellis , Michael Palte
IPC分类号： C07K19/00
CPC分类号： C12N9/2462 , A61K47/54 , C07F5/025 , C12N9/22 , C12Y301/27005 , C12Y302/01017
摘要： Methods for enhancing cellular uptake of cargo molecules by boronating the cargo molecule, particularly with one or more phenylboronic acid groups. Cellular uptake includes at least partial uptake into the cytosol. Boronation includes ligating, crosslinking or otherwise bonding one or more phenylboronic acids substituted to contain a reactive group to a cargo molecule. Boronation also includes ligating, crosslinking or otherwise bonding a phenylboronated oligopeptide to a cargo molecule. The phenylboronate groups are optionally conjugated to the cargo molecule via linking moieties that can be selectively cleaved, such cleavable linkers can allow the phenylboronate groups to be removed from the cargo molecule after the boronated cargo molecule is introduced into the cell. The invention includes certain phenylboronates which are boronation reagents, certain boronated oligopeptides and certain boronated peptides and proteins. The invention also includes kits for enhancing cellular uptake of cargo molecules by boronation with one or more phenylboronates or boronated oligopeptides.
摘要翻译： 通过将货物分子，特别是与一个或多个苯基硼酸基团进行硼化来增强货物分子的细胞吸收的方法。 细胞摄取包括至少部分摄入胞质溶胶。 硼化包括连接，交联或以其他方式将一个或多个被取代以含有反应性基团的苯基硼酸与货物分子结合。 硼化还包括将苯基硼化寡肽与货物分子结合，交联或以其它方式结合。 苯硼酸酯基团任选地通过可以选择性切割的连接部分缀合到货物分子，这种可切割接头可以在硼化货物分子被引入细胞后允许苯基硼酸酯基团从货物分子中除去。 本发明包括某些苯硼氢化物，其为硼化试剂，某些硼化寡肽和某些硼化肽和蛋白质。 本发明还包括用于通过硼化与一种或多种苯基硼酸盐或硼化寡肽来增强货物分子的细胞摄取的试剂盒。
-
公开(公告)号：US08410247B2
公开(公告)日：2013-04-02
申请号：US12546249
申请日：2009-08-24
申请人： Ronald T. Raines , Annie Tam , Matthew B. Soellner
发明人： Ronald T. Raines , Annie Tam , Matthew B. Soellner
IPC分类号： C07C231/10 , C07F9/50 , C07K1/02 , C07K1/04
CPC分类号： C07K1/082 , C07F9/5004 , C07F9/5022 , C07K1/086
摘要： Water soluble reagents and methods for the formation of an amide bond between a phosphinothioester and an azide in an aqueous medium. The phosphinothioester is generated using a water-soluble phosphinothiol reagent. This reaction allows formation of an amide bond between a wide variety of chemical species including amino acids, peptides or protein fragments in an aqueous solution. Of particular interest, this reaction allows for the formation of an amide bond in a physiological setting. In a specific embodiment, this invention provides reagents and methods for peptide ligation in an aqueous medium. The reaction eliminates the need for a cysteine residue and is traceless leaving no residual atoms in the ligated peptide product.
摘要翻译： 水溶性试剂和在水性介质中在膦硫基酯和叠氮化物之间形成酰胺键的方法。 使用水溶性硫代硫醇试剂产生膦硫代酯。 该反应允许在各种各样的化学物质（包括水溶液中的氨基酸，肽或蛋白质片段）之间形成酰胺键。 特别令人感兴趣的是，该反应允许在生理环境中形成酰胺键。 在具体实施方案中，本发明提供了用于在水性介质中肽连接的试剂和方法。 该反应消除了对半胱氨酸残基的需要，并且在连接的肽产物中没有残留的原子。
-
公开(公告)号：US20120009173A1
公开(公告)日：2012-01-12
申请号：US13243373
申请日：2011-09-23
摘要： This invention relates to cytotoxic variants of human ribonuclease 1 (RNase 1) identified through analysis of the interaction between RNase 1 and the human ribonuclease inhibitor (hRI) as defined by the three dimensional (3-D) atomic structure of the RNase1 hRI complex. Also disclosed is the 3-D structure of the hRI•RNase 1 complex and methods for designing the RNase 1 variants.
摘要翻译： 本发明涉及通过分析由RNase1 hRI复合物的三维（3-D）原子结构定义的核糖核酸酶1和人核糖核酸酶抑制剂（hRI）之间的相互作用而鉴定的人核糖核酸酶1（核糖核酸酶1）的细胞毒性变体。 还公开了hRI·RNase 1复合物的3-D结构和用于设计RNA酶1变体的方法。
-
公开(公告)号：US07973132B2
公开(公告)日：2011-07-05
申请号：US12245546
申请日：2008-10-03
申请人： Ronald T. Raines , Stephen M. Fuchs
发明人： Ronald T. Raines , Stephen M. Fuchs
CPC分类号： C12Q1/37 , C07K14/43595 , G01N33/5005
摘要： This invention relates to methods and compositions for designing novel fluorescent proteins, preferably to a green fluorescent proteins (GFP). The engineered GFPs are modified by substituting negatively charged amino acids with positively charged amino acids on the exterior of the protein making the protein cell permeable. The ability of the engineered fluorescent proteins to permeate cells obviates the need for transfections, allowing these novel proteins to be used in numerous biological applications.
摘要翻译： 本发明涉及用于设计新的荧光蛋白，优选绿色荧光蛋白（GFP）的方法和组合物。 通过在蛋白质外部用带正电荷的氨基酸取代带负电荷的氨基酸来修饰工程化的GFP，使得蛋白质细胞是可渗透的。 工程化荧光蛋白渗透细胞的能力消除了转染的需要，允许这些新型蛋白质用于许多生物应用。
-
-
-
-
-
-
-
-
-
搜索结果
55 条记录 (耗时 0.036 秒)
