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1. 发明申请

WO2013024144A1 MARKERS FOR SUSCEPTIBILITY TO AN INHIBITOR OF AN SRC-FAMILY KINASE 审中-公开
标题翻译：不符合SRC家族激素抑制剂的标记
公开(公告)号：WO2013024144A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/066055
申请日：2012-08-16
申请人： EVOTEC (MÜNCHEN) GMBH , SCHAAB, Christoph , GODL, Klaus , KLAMMER, Martin , TEBBE, Andreas , MÜLLER, Stefan
发明人： SCHAAB, Christoph , GODL, Klaus , KLAMMER, Martin , TEBBE, Andreas , MÜLLER, Stefan
IPC分类号： G01N33/50
CPC分类号： C12Q1/6881 , G01N33/56966 , G01N33/574 , G01N2333/70546
摘要： The present invention relates to a method for predicting the responsiveness of a mammalian tumor cell or cancer cell to an inhibitor of a kinase of the Src family, such as dasatinib, bosutinib. saracitinib or ponatinib. The present invention also provides for a method for predicting the responsiveness of an individual to an inhibitor of a kinase of the Src family, whereby the individual is suspected to suffer from cancer. These methods involve the evaluation of the status of integrin β4, wherein said status is indicative for the responsiveness to the inhibitor. Furthermore, a kit useful for carrying out the methods described herein as well as an oligo- or polynucleotide and/or antibodies capable of detecting the expression level of integrin β4 for predicting the responsiveness to the inhibitor are provided.
摘要翻译：本发明涉及一种用于预测哺乳动物肿瘤细胞或癌细胞对Src家族的激酶抑制剂如达沙替尼（basutinib）的反应性的方法。沙拉替尼或帕那他滨。本发明还提供了一种用于预测个体对Src家族的激酶抑制剂的反应性的方法，由此该个体怀疑患有癌症。这些方法包括评估整合素β4的状态，其中所述状态指示对抑制剂的反应性。此外，提供了可用于实施本文所述方法的试剂盒以及能够检测整合素β4的表达水平以预测对抑制剂的反应性的寡核苷酸和/或多核苷酸和/或抗体。

2. 发明申请

WO2009043829A1 PROTEOME-WIDE QUANTIFICATION OF SMALL MOLECULE BINDING TO CELLULAR TARGET PROTEINS 审中-公开
标题翻译：小分子结合细胞靶向蛋白的广泛定量
公开(公告)号：WO2009043829A1
公开(公告)日：2009-04-09
申请号：PCT/EP2008/062979
申请日：2008-09-26
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. , DAUB, Henrik , BAIRLEIN, Michaela , SHARMA, Kirti , GODL, Klaus , TEBBE, Andreas , WEBER, Christoph
发明人： DAUB, Henrik , BAIRLEIN, Michaela , SHARMA, Kirti , GODL, Klaus , TEBBE, Andreas , WEBER, Christoph
IPC分类号： C12Q1/48 , G01N33/543 , G01N33/68
CPC分类号： G01N33/54306 , C12Q1/485 , G01N30/6043 , G01N30/7233 , G01N30/8675 , G01N33/6851
摘要： This invention relates to methods for the evaluation and/or quantification of the binding affinity of small molecules or other compounds to target components contained within an analyte, such as target proteins contained within the proteome of a cell or tissue.
摘要翻译：本发明涉及用于评估和/或定量小分子或其它化合物对分析物中所含的靶组分（例如包含在细胞或组织的蛋白质组中的靶蛋白）的结合亲和力的方法。

3. 发明申请

WO2014087018A1 MARKERS FOR RESPONSIVENESS TO AN INHIBITOR OF FLT3 审中-公开
标题翻译：对FLT3抑制剂的反应标记
公开(公告)号：WO2014087018A1
公开(公告)日：2014-06-12
申请号：PCT/EP2013/075970
申请日：2013-12-09
申请人： EVOTEC (MÜNCHEN) GMBH
发明人： SCHAAB, Christoph , GODL, Klaus , OPPERMANN, Felix S. , KLAMMER, Martin , TEBBE, Andreas , SERVE, Hubert
IPC分类号： G01N33/574 , G01N33/68
CPC分类号： G01N33/574 , G01N2333/912
摘要： The present invention relates to methods of determining whether a proliferative diseased cell is responsive to an FMS-like tyrosine kinase 3 (FLT3) inhibitor, like quizartinib (AC220). The methods comprise determining the phosphorylation status of B-cell lymphoma/leukemia 11A protein (BCL1 1A), Lamin A/C (LMN1), endonuclease/exonuclease/phosphatase family domain- containing protein 1 (EEPD1), Ran-binding protein 3 (RANBP3), and/or GTPase regulator (RP3) in a sample of a patient, wherein the phosphorylation status is indicative of responsiveness to FLT3 inhibitor. The patient can suffer from neoplasia, like AML. Also the therapeutic use of FLT3 inhibitors (like quizartinib (AC220)) in the treatment of patients determined to have a specific phosphorylation status is provided.
摘要翻译：本发明涉及确定增殖性疾病细胞是否对FMS样酪氨酸激酶3（FLT3）抑制剂（如比卡替尼（AC220））起反应的方法。该方法包括测定B细胞淋巴瘤/白血病11A蛋白（BCL1A1），Lamin A / C（LMN1），内切核酸酶/核酸外切核酸酶/磷酸酶家族域蛋白1（EEPD1），Ran结合蛋白3（ RANBP3）和/或GTP酶调节剂（RP3），其中磷酸化状态指示对FLT3抑制剂的反应性。患者可能患有肿瘤，如AML。此外，还提供了FLT3抑制剂（如考亚胺（AC220））在治疗确定具有特定磷酸化状态的患者中的治疗用途。

4. 发明申请

WO2004013633A2 MEDIUM AND METHOD FOR ENRICHING, PURIFYING OR DEPLETING ATP BINDING PROTEINS FROM A POOL OF PROTEINS 审中-公开
标题翻译：从蛋白质池中增殖，净化或减少ATP结合蛋白的培养基和方法
公开(公告)号：WO2004013633A2
公开(公告)日：2004-02-12
申请号：PCT/EP2003/008375
申请日：2003-07-29
申请人： AXXIMA PHARMACEUTICALS AG , GODL, Klaus , MISSIO, Andrea , DAUB, Henrik , STEIN-GERLACH, Matthias , GREFF, Zoltan
发明人： GODL, Klaus , MISSIO, Andrea , DAUB, Henrik , STEIN-GERLACH, Matthias , GREFF, Zoltan
IPC分类号： G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/6803 , G01N2333/91205
摘要： The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-l H -imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8 H -pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1 H -indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-3-(1 H -indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-4-(1-methyl-l H -indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2- a ]-indol-10-yl)-4-(1-methyl-l H -indol -3-y1)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-l-yl-methyl]- N -[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases from a pool of heterogeneous proteins.
摘要翻译：本发明涉及一种培养基和一种富含ATP结合蛋白的方法，蛋白质蛋白酶，来自蛋白质库，如蛋白质组。本发明的培养基包含特异性抑制剂，例如， 4- [4-（4-氟 - 苯基）-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺中的至少一种化合物，2- [4-（2-氨基 - 乙氧基） - 苯基氨基] -6-（2,6-二氯 - 苯基）-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮，2- [1-（3-氨基丙基）-1H-吲哚 -3-基）马来酰亚胺，3- [1-（3-氨基丙基）-1H-吲哚-3-基] -3-（1H-吲哚-3-基） - 马来酰亚胺，3- [1-（3-氨基丙基） -1H-吲哚-3-基] -4-（1-甲基-1H-吲哚-3-基）马来酰亚胺，3-（8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a ] - （1-甲基-1H-吲哚-3-基） - 马来酰胺，[6-（3-氨基 - 丙氧基） - 甲氧基 - 喹唑啉-4-基] - （3- 苯基） - 胺，6-（3-氨基 - 丙氧基）-7-甲氧基 - 喹唑啉-4-基 - （3-氯-4-氟 - 苯基） - 胺，6-（3Amino-丙氧基） - -7-甲氧基 - 喹唑啉-4-基] - （3-溴 - 苯基） - 胺和4- [4-（4-氨基 - 丁基） - 哌嗪-1-基 - 甲基] -N- [4-甲基 - 3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺固定在载体材料上。根据本发明的方法，上述固定化化合物用于选择性地结合来自异质蛋白库的蛋白激酶。

5. 发明公开

EP2745113A1 MARKERS FOR SUSCEPTIBILITY TO AN INHIBITOR OF AN SRC-FAMILY KINASE 有权
标题翻译： MARKER灵敏度一个抑制剂SRC激酶家族
公开(公告)号：EP2745113A1
公开(公告)日：2014-06-25
申请号：EP12758419.1
申请日：2012-08-16
申请人： Evotec (München) GmbH
发明人： SCHAAB, Christoph , GODL, Klaus , KLAMMER, Martin , TEBBE, Andreas , MÜLLER, Stefan
IPC分类号： G01N33/50
CPC分类号： C12Q1/6881 , G01N33/56966 , G01N33/574 , G01N2333/70546
摘要： The present invention relates to a method for predicting the responsiveness of a mammalian tumor cell or cancer cell to an inhibitor of a kinase of the Src family, such as dasatinib, bosutinib. saracitinib or ponatinib. The present invention also provides for a method for predicting the responsiveness of an individual to an inhibitor of a kinase of the Src family, whereby the individual is suspected to suffer from cancer. These methods involve the evaluation of the status of integrin β4, wherein said status is indicative for the responsiveness to the inhibitor. Furthermore, a kit useful for carrying out the methods described herein as well as an oligo- or polynucleotide and/or antibodies capable of detecting the expression level of integrin β4 for predicting the responsiveness to the inhibitor are provided.

6. 发明授权

EP2745113B1 MARKERS FOR SUSCEPTIBILITY TO AN INHIBITOR OF AN SRC-FAMILY KINASE 有权
标题翻译： MARKERFÜRDIEANFÄLLIGKEITFÜREINEN HEMMER EINER SRC-KINASEFAMILIE
公开(公告)号：EP2745113B1
公开(公告)日：2017-03-22
申请号：EP12758419.1
申请日：2012-08-16
申请人： Evotec (München) GmbH
发明人： SCHAAB, Christoph , GODL, Klaus , KLAMMER, Martin , TEBBE, Andreas , MÜLLER, Stefan
IPC分类号： G01N33/50
CPC分类号： C12Q1/6881 , G01N33/56966 , G01N33/574 , G01N2333/70546

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