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1. 发明申请

WO2012143714A1 METHODS FOR DETERMINING LIGAND BINDING TO A TARGET PROTEIN USING A THERMAL SHIFT ASSAY 审中-公开
标题翻译：使用热转移测定法测定配体蛋白质的目标蛋白质的方法
公开(公告)号：WO2012143714A1
公开(公告)日：2012-10-26
申请号：PCT/GB2012/050853
申请日：2012-04-18
申请人： EVITRAPROTEOMA AB , NORDLUND, Pär , GARDNER, Rebecca
发明人： NORDLUND, Pär
IPC分类号： G01N33/68
CPC分类号： G01N33/6803 , G01N33/68 , G01N33/6845 , G01N33/9446 , G01N33/9453 , G01N33/946 , G01N33/9466 , G01N33/9473 , G01N33/948 , G01N33/9486 , G01N33/9493
摘要： The invention is directed to a method of determining whether a non-purified sample contains a target protein bound to a ligand of interest comprising the steps of: a) exposing said non-purified sample to a temperature which is capable of causing or enhancing precipitation of the unbound target protein to a greater extent than it is capable of causing or enhancing precipitation of the target protein bound to said ligand; b) processing the product of step a) in order to separate soluble from insoluble protein; and c) analysing either or both the soluble and insoluble protein fractions of step b) for the presence of target protein, wherein said target protein is not detected on the basis of enzymatic activity of a tag, peptide, polypeptide or protein fused thereto. Particularly, the invention may be used to determine whether drugs can bind to their protein targets in samples derived from patients to ascertain whether a certain drug can be used in a therapy for that patient. Additionally, the invention is directed to an instrument for use in the methods of the invention and use of a kit in the methods of the invention comprising an antibody and/or a non-protein fusion tag.
摘要翻译：本发明涉及一种确定非纯化样品是否含有与感兴趣配体结合的靶蛋白的方法，包括以下步骤：a）将所述未纯化样品暴露于能够引起或增强沉淀的温度未结合的靶蛋白比其能够引起或增强结合到所述配体的靶蛋白的沉淀更大程度; b）加工步骤a）的产物，以分离可溶性不溶蛋白质; 和c）分析步骤b）的可溶性和不溶性蛋白质级分中的一种或两种，以确定靶蛋白的存在，其中基于与其融合的标签，肽，多肽或蛋白质的酶活性，未检测到所述靶蛋白。特别地，本发明可用于确定药物是否可以结合其衍生自患者的样品中的蛋白质靶标，以确定某种药物是否可用于该患者的治疗。另外，本发明涉及用于本发明方法的仪器，并且在包含抗体和/或非蛋白质融合标签的本发明方法中使用试剂盒。

2. 发明申请

WO2005003784A1 A METHOD OF SCREENING FOR CELL COLONIES THAT EXPRESS A SOLUBLE VARIANT OF A TARGET PROTEIN 审中-公开
标题翻译：筛选表达目标蛋白的可溶性变体的细胞系的方法
公开(公告)号：WO2005003784A1
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002271
申请日：2004-05-27
申请人： GARDNER, Rebecca , NORDLUND, Pär , CORNVIK, Tobias , DAHLROTH, Sue-Li , KNAUST, Rose-Marie
发明人： NORDLUND, Pär , CORNVIK, Tobias , DAHLROTH, Sue-Li , KNAUST, Rose-Marie
IPC分类号： G01N33/68
CPC分类号： G01N33/6842
摘要： The present invention concerns a method of identifying a cell colony which expresses a soluble variant of a target protein which method comprises (a) subjecting the cell colony to conditions which are capable of causing lysis thereof; (b) filtering the lysate through a filter having pores which allow only soluble proteins to pass through the filter; and (c) detecting target protein which has passed through the filter where the target is not detected an the basis of its own enzymatic activity. The invention further covers the identification of a cell colony expressing a soluble variant of a membrane protein using steps (a) and (b) of the method above. A kit for use in the methods is also covered by the invention.
摘要翻译：本发明涉及鉴定表达靶蛋白的可溶性变体的细胞集落的方法，该方法包括（a）使细胞集落受到能够引起其裂解的条件; （b）通过具有仅允许可溶性蛋白质通过过滤器的孔的过滤器来过滤裂解物; 和（c）检测已经通过过滤器的靶蛋白，其中靶没有被检测到其本身的酶活性的基础。本发明进一步包括使用上述方法的步骤（a）和（b）来鉴定表达膜蛋白的可溶性变体的细胞集落。用于该方法的试剂盒也被本发明覆盖。

3. 发明申请

WO2008142366A2 METHODS 审中-公开
标题翻译：方法
公开(公告)号：WO2008142366A2
公开(公告)日：2008-11-27
申请号：PCT/GB2008/001584
申请日：2008-05-07
申请人： BIOLIPOX AB , MCNEENEY, Stephen, Phillip , KOHL, Andreas , ESHAGHI, Said , MOLINA, Daniel, Martinez , NORDLUND, Pär , WETTERHOLM, Anders , HAEGGSTRÖM, Jesper, Z.
发明人： KOHL, Andreas , ESHAGHI, Said , MOLINA, Daniel, Martinez , NORDLUND, Pär , WETTERHOLM, Anders , HAEGGSTRÖM, Jesper, Z.
IPC分类号： G06F19/00
CPC分类号： C12Q1/25 , C07K2299/00 , C12N9/1085 , C12Y404/0102 , G01N33/92 , G01N2500/04 , G06F19/16
摘要： A method for selecting or designing a compound expected to modulate the activity of Leukotriene C4 synthase (LTC4S), the method comprising the step of using molecular modelling means to select or design a compound that is predicted to interact with the catalytic site or a substrate binding region of LTC4S, wherein a three-dimensional structure of at least a part of the catalytic site or a substrate binding region of LTC4S is compared with a three-dimensional structure of a compound, and a compound that is predicted to interact with the said catalytic site or substrate binding region is selected. The selected compound may be predicted to bind to at least a part of a region of the structure termed the "GSH substrate binding cavity" (formed by residues including residues Arg51, Arg30, Arg104, Gln53, Asn55, Glu58, Tyr59, Tyr93, Tyr97, Ile27, Pro37, Leu108 of full length human LTC4S, or equivalent residues); the "lipophilic substrate binding crevice" (formed by residues including Ala20, Leu24, Ile27, Tyr59, Trp116, Ala112, Leu115, Leu108, Tyr109, Leu62, VaI119, Thr66, Val119 and Leu17, or equivalent residues); or the "catalytic site" (formed by residues including Arg104 or Arg31, or equivalent residues).
摘要翻译：选择或设计预期调节白三烯C4合酶（LTC4S）的活性的化合物的方法，所述方法包括使用分子建模手段来选择或设计预测与催化位点相互作用的化合物或底物结合 LTC4S的区域，其中将LTC4S的至少一部分催化位点或底物结合区域的三维结构与化合物的三维结构进行比较，以及预测与所述催化剂相互作用的化合物选择位点或底物结合区。可以预期所选择的化合物可结合称为“GSH底物结合腔”的结构的至少一部分（由残基Arg51，Arg30，Arg104，Gln53，Asn55，Glu58，Tyr59，Tyr93，Tyr97 ，全长人LTC4S的Ile27，Pro37，Leu108或相当的残基）; （由Ala20，Leu24，Ile27，Tyr59，Trp116，Ala112，Leu115，Leu108，Tyr109，Leu62，Val119，Thr66，Val119和Leu17等残基组成的“亲脂性底物结合缝隙”）。或“催化位点”（由包含Arg104或Arg31的残基或等同残基形成）。

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