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    SELF-CELL PENETRATING FLUORESCENT PEPTIDE BIOSENSORS TO PROBE AND QUANTIFY CDK/CYCLIN KINASES
    1.
    发明申请
    SELF-CELL PENETRATING FLUORESCENT PEPTIDE BIOSENSORS TO PROBE AND QUANTIFY CDK/CYCLIN KINASES 审中-公开
    自体细胞培养荧光肽生物传感器探测和定量CDK / CYCLIN KINASES

    公开(公告)号：WO2014147191A1

    公开(公告)日：2014-09-25

    申请号：PCT/EP2014/055631

    申请日：2014-03-20

    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES

    Inventor： MORRIS, May, Catherine ,  KURZAWA, Laeticia ,  PELLERANO, Morgan

    IPC: G01N33/573 ,  C07K7/00 ,  G01N33/58

    CPC classification number: C07K14/4738 ,  C07K7/08 ,  C12N9/1205 ,  G01N33/573 ,  G01N33/582 ,  G01N2333/4739 ,  G01N2333/912

    Abstract: The present invention relates to compounds comprising a polypeptide and a fluorophore, said said compounds being able to penetrate directly into living cells and to bind to CDK/Cyclin complexes. Compounds according to the invention are therefore able to probe the relative abundance of these protein complexes. The present invention also relates to a method for determining the presence of CDK/Cyclin complexes in cell samples through a ratiometric quantitation strategy using compounds according to the invention. The invention finally relates to the use of said compounds and/or of compositions comprising said compounds for in vitro detecting the presence and/or the level of expression of CDK/Cyclin complexes, for high throughput and high content screening of libraries of compounds and for medical imaging.

    Abstract translation: 本发明涉及包含多肽和荧光团的化合物，所述化合物能够直接渗入活细胞并结合CDK /细胞周期蛋白复合物。 因此，根据本发明的化合物能够探测这些蛋白质复合物的相对丰度。 本发明还涉及通过使用根据本发明的化合物的比例定量策略来测定细胞样品中CDK /细胞周期蛋白复合物的存在的方法。 本发明最终涉及所述化合物和/或包含所述化合物的组合物用于体外检测CDK /细胞周期蛋白复合物的存在和/或水平的用途，用于化合物文库的高通量和高含量筛选 医学影像。

    GENERATION OF MITOTIC PHASE REPORTER FOR IN VIVO BIOLUMINESCENCE IMAGING IN LIVING ANIMALS
    3.
    发明申请
    GENERATION OF MITOTIC PHASE REPORTER FOR IN VIVO BIOLUMINESCENCE IMAGING IN LIVING ANIMALS 审中-公开
    生物动物生物相容性生物识别的生成

    公开(公告)号：WO2010042333A1

    公开(公告)日：2010-04-15

    申请号：PCT/US2009/058515

    申请日：2009-09-28

    Applicant: MERCK SHARP & DOHME CORP. ,  ZHANG, Guy-Jun ,  SUR, Cyrille

    Inventor： ZHANG, Guy-Jun ,  SUR, Cyrille

    IPC: C12N15/00 ,  C12P21/06 ,  C12P21/04 ,  A61K39/00

    CPC classification number: G01N33/5011 ,  G01N2333/4739 ,  G01N2333/90241 ,  G01N2510/00

    Abstract: Disclosed herein is a fusion protein comprising of 173 amino acid residues of the N terminus of cyclin B1 (including the Destruction Box and Cytoplasmic Retention Signal) fused in-frame with the luciferase reporter gene. Expression of the fusion protein is driven by the cyclin B1 promoter and mimics expression of the endogenous cyclin B1 gene. Following addition of the substrate luciferin, increased levels of the luciferase reporter gene can be used to monitor cell cycle arrest at the G2/M phase. Importantly, this invention may be used in vivo to monitor luciferase expression and G2/M cell cycle arrest in living animals. A broad aspect of the invention provides a method of detecting cell death in a target cell comprising transfecting the target cell with a nucleic acid construct that encodes a cyclinB1-Luciferase fusion protein under conditions favoring expression of the fusion protein; introducing the target cell with a substrate specific for the fusion protein for a period of time sufficient to detect a signal, wherein the generation of a signal indicates that the cell has arrested at the G2/M transition; and detecting a signal.

    Abstract translation: 本文公开了一种融合蛋白，其包含与萤光素酶报告基因框架融合的细胞周期蛋白B1（包括破坏盒和细胞质保留信号）的N末端的173个氨基酸残基。 融合蛋白的表达由细胞周期蛋白B1启动子驱动并模拟内源性细胞周期蛋白B1基因的表达。 添加底物萤光素后，荧光素酶报告基因的增加可用于监测G2 / M期的细胞周期停滞。 重要的是，本发明可以在体内用于监测活的动物中的荧光素酶表达和G2 / M细胞周期停滞。 本发明的广泛方面提供了一种检测靶细胞中的细胞死亡的方法，包括在有利于融合蛋白表达的条件下用编码细胞周期蛋白B1荧光素酶融合蛋白的核酸构建体转染靶细胞; 将具有融合蛋白特异性底物的靶细胞引入足以检测信号的时间段，其中信号的产生指示细胞在G2 / M转变处已经停止; 并检测信号。

    EIF4E REGULON-BASED DIAGNOSTICS
    5.
    发明申请
    EIF4E REGULON-BASED DIAGNOSTICS 审中-公开
    基于EIF4E REGULON的诊断

    公开(公告)号：WO2008060369A2

    公开(公告)日：2008-05-22

    申请号：PCT/US2007021167

    申请日：2007-10-01

    Applicant: TRANSLATIONAL THERAPEUTICS ,  JAMIESON GORDON A ,  BORDEN KATHERINE L B

    Inventor： JAMIESON GORDON A ,  BORDEN KATHERINE L B

    IPC: G01N33/53

    CPC classification number: G01N33/57484 ,  G01N33/5011 ,  G01N2333/4703 ,  G01N2333/4739 ,  G01N2510/00 ,  G01N2800/32

    Abstract: Provided are methods and compositions for the identification, diagnosis and monitoring of 4E regulon activity and for the discovery of agents that modulate 4E regulon activity. The methods, compositions and agents may be used alone, in combination with or in conjunction with other therapies for the detection and treatment of diseases wherein 4E regulon activity is dysfunctional, including cellular hypertrophy, cancer, and ischemia reperfusion.

    Abstract translation: 提供了用于鉴定，诊断和监测4E调节子活性和用于发现调节4E调节子活性的药剂的方法和组合物。 所述方法，组合物和药剂可以单独使用，与其他治疗组合或联合用于检测和治疗其中4E调节子活性失调的疾病，包括细胞肥大，癌症和缺血再灌注。

    CYCLIN GROOVE INHIBITORS
    6.
    发明申请
    CYCLIN GROOVE INHIBITORS 审中-公开
    CYCLIN GROVE抑制剂

    公开(公告)号：WO2005042565A3

    公开(公告)日：2005-08-11

    申请号：PCT/GB2004004454

    申请日：2004-10-21

    Applicant: CYCLACEL LTD ,  ANDREWS MARTIN J I ,  MCINNES CAMPBELL ,  KONTOPIDIS GEORGE ,  FISCHER PETER M

    Inventor： ANDREWS MARTIN J I ,  MCINNES CAMPBELL ,  KONTOPIDIS GEORGE ,  FISCHER PETER M

    IPC: A61K38/00 ,  C07K14/47 ,  G01N33/50 ,  G01N33/68 ,  C07K5/00 ,  C07K5/02 ,  C07K7/00 ,  C07K7/02 ,  G01N33/574 ,  G06F19/00

    CPC classification number: C07K14/4738 ,  A61K38/00 ,  G01N33/5011 ,  G01N33/6872 ,  G01N2333/4739 ,  G01N2333/91205 ,  G01N2500/02

    Abstract: The present invention relates to a compound of formula (I), or a variant thereof, A - (B)m - C - (D)n- E, wherein m and n are each independently 0 or 1 and A, B, C, D and E are each independently linked to the respective adjacent residue by a linker group independently selected from carboxamide, reduced carboxamide, sulfonamide, imine, semicarbazone, oxime and ethanolamine; A is (i) a natural or unnatural amino acid residue having a side chain comprising at least one H-bond acceptor moiety and at least one H-bond donor moiety, or a derivative thereof; or (ii) R(CO), wherein R is a C1-C24 hydrocarbyl group comprising at least one H-bond acceptor moiety and optionally one or more H-bond donor moieties, and where R optionally contains one or more heteroatoms selected from S, O, and N, and is optionally substituted by one or more substituents selected from halogen, OMe, CN, CF3, and NO2; each of B and D is independently an amino acid residue selected from arginine, 4-(guanidinyl)phenylalanine (4-(Gu)Phe), piperidinylglycine (PipGly), piperidinylalanine (PipAla), pyridinylalanine, histamine, N,N-(dimethyl) lysine (DMLys), citrulline, glutamine, serine, lysine, asparagine, isoleucine and alanine, or a derivative thereof; C is NH-X-CO, where X is a C1-C4 alkylene group substituted by a straight-chain or branched C1-C6 alkylene group, said C1-C6 alkylene group optionally containing a H-bond donor or H-bond acceptor moiety; E is (i) a natural or unnatural amino acid residue having an aryl or heteroaryl side chain, or a derivative thereof; or (ii) NHR', where R' is a C1-C24 hydrocarbyl group, optionally containing one or more heteroatoms selected from N, O, and S, and optionally comprising one or more H-bond acceptor or donor moieties; said hydrocarbyl group further comprising a pendent C4-C12 aryl or heteroaryl group, which itself may be optionally substituted by one or more substituents selected from a H-bond donor moiety, a H-bond acceptor moiety, a halogen, Me, Et, Pr, CF3, CN and NO2; wherein at least one of A and E is other than a natural or unnatural amino acid residue when A, B, C, D and E are each linked to the respective adjacent residue by a carboxamide group.

    Abstract translation: 本发明涉及式（I）化合物或其变体，A - （B）m -C-（D）n-E，其中m和n各自独立地为0或1，A，B，C D和E各自独立地通过独立地选自羧酰胺，还原羧酰胺，磺酰胺，亚胺，缩氨基脲，肟和乙醇胺的连接基团相应地相邻的相邻残基连接。 A是（i）具有侧链的天然或非天然氨基酸残基，所述侧链包含至少一个H键受体部分和至少一个H键供体部分或其衍生物; 或（ii）R（CO），其中R是包含至少一个H键受体部分和任选的一个或多个H键供体部分的C 1 -C 24烃基，并且其中R任选地含有一个或多个选自S ，O和N，并且任选地被一个或多个选自卤素，OMe，CN，CF 3和NO 2的取代基取代; B和D中的每一个独立地为选自精氨酸，4-（胍基）苯丙氨酸（4-（Gu）Phe），哌啶基甘氨酸（PipGly），哌啶基丙氨酸（PipAla），吡啶丙氨酸，组胺，N，N- ）赖氨酸（DMLys），瓜氨酸，谷氨酰胺，丝氨酸，赖氨酸，天冬酰胺，异亮氨酸和丙氨酸或其衍生物; C是NH-X-CO，其中X是被直链或支链C1-C6亚烷基取代的C1-C4亚烷基，所述C1-C6亚烷基任选地含有H-键供体或H-键受体部分 ; E是（i）具有芳基或杂芳基侧链的天然或非天然氨基酸残基或其衍生物; 或（ii）NHR'，其中R'是C 1 -C 24烃基，任选地含有一个或多个选自N，O和S的杂原子，并任选地包含一个或多个H键受体或供体部分; 所述烃基还包含悬挂的C 4 -C 12芳基或杂芳基，其本身可以任选地被一个或多个选自H键供体部分，H-键受体部分，卤素，Me，Et，Pr ，CF3，CN和NO2; 其中当A，B，C，D和E各自通过羧酰胺基团连接到相应的相邻残基时，A和E中的至少一个不是天然或非天然氨基酸残基。

    CYCLIN GROOVE INHIBITORS
    7.
    发明申请
    CYCLIN GROOVE INHIBITORS 审中-公开
    CYCLIN凹槽抑制剂

    公开(公告)号：WO2005042565A2

    公开(公告)日：2005-05-12

    申请号：PCT/GB2004/004454

    申请日：2004-10-21

    Applicant: CYCLACEL LIMITED ,  ANDREWS, Martin, J., I. ,  MCINNES, Campbell ,  KONTOPIDIS, George ,  FISCHER, Peter, M.

    Inventor： ANDREWS, Martin, J., I. ,  MCINNES, Campbell ,  KONTOPIDIS, George ,  FISCHER, Peter, M.

    IPC: C07K5/00

    CPC classification number: C07K14/4738 ,  A61K38/00 ,  G01N33/5011 ,  G01N33/6872 ,  G01N2333/4739 ,  G01N2333/91205 ,  G01N2500/02

    Abstract: The present invention relates to a compound of formula (I), or a variant thereof, A - (B) m - C - (D) n - E, wherein m and n are each independently 0 or 1 and A, B, C, D and E are each independently linked to the respective adjacent residue by a linker group independently selected from carboxamide, reduced carboxamide, sulfonamide, imine, semicarbazone, oxime and ethanolamine; A is (i) a natural or unnatural amino acid residue having a side chain comprising at least one H-bond acceptor moiety and at least one H-bond donor moiety, or a derivative thereof; or (ii) R(CO), wherein R is a C 1 -C 24 hydrocarbyl group comprising at least one H-bond acceptor moiety and optionally one or more H-bond donor moieties, and where R optionally contains one or more heteroatoms selected from S, O, and N, and is optionally substituted by one or more substituents selected from halogen, OMe, CN, CF 3 , and NO 2 ; each of B and D is independently an amino acid residue selected from arginine, 4-(guanidinyl)phenylalanine (4-(Gu)Phe), piperidinylglycine (PipGly), piperidinylalanine (PipAla), pyridinylalanine, histamine, N,N -(dimethyl) lysine (DMLys), citrulline, glutamine, serine, lysine, asparagine, isoleucine and alanine, or a derivative thereof; C is NH-X-CO, where X is a C 1 -C 4 alkylene group substituted by a straight-chain or branched C 1 -C 6 alkylene group, said C 1 -C 6 alkylene group optionally containing a H-bond donor or H-bond acceptor moiety; E is (i) a natural or unnatural amino acid residue having an aryl or heteroaryl side chain, or a derivative thereof; or (ii) NHR’, where R’ is a C 1 -C 24 hydrocarbyl group, optionally containing one or more heteroatoms selected from N, O, and S, and optionally comprising one or more H-bond acceptor or donor moieties; said hydrocarbyl group further comprising a pendent C 4 -C 12 aryl or heteroaryl group, which itself may be optionally substituted by one or more substituents selected from a H-bond donor moiety, a H-bond acceptor moiety, a halogen, Me, Et, i Pr, CF 3 , CN and NO 2 ; wherein at least one of A and E is other than a natural or unnatural amino acid residue when A, B, C, D and E are each linked to the respective adjacent residue by a carboxamide group.

    Abstract translation: 本发明涉及式（I）化合物或其变体，A - （B）m -C（D）n - 其中m和n各自独立地为0或1，并且A，B，C，D和E各自独立地通过独立选自甲酰胺，还原的甲酰胺，磺酰胺，亚胺 ，缩氨基脲，肟和乙醇胺; A是（i）具有包含至少一个H-键受体部分和至少一个H-键供体部分或其衍生物的侧链的天然或非天然氨基酸残基; 或（ii）R（CO），其中R是包含至少一个H-键受体部分的C 1 -C 24烃基和任选地一个或多个H- 键供体部分，并且其中R任选地含有一个或多个选自S，O和N的杂原子，并且任选地被一个或多个选自卤素，OMe，CN，CF 3和 NO <子> 2 ; 每个B和D独立地选自精氨酸，4-（胍基）苯丙氨酸（4-（Gu）Phe），哌啶基甘氨酸（PipGly），哌啶基丙氨酸（PipAla），吡啶基丙氨酸，组胺，N，N （二甲基）赖氨酸（DMLys），瓜氨酸，谷氨酰胺，丝氨酸，赖氨酸，天冬酰胺，异亮氨酸和丙氨酸或其衍生物; C是NH-X-CO，其中X是被直链或支链C 1 -C 4烷基取代的C 1 -C 4亚烷基， -C≡6亚烷基，所述C 1 -C 6亚烷基任选地含有H键供体或H键受体部分; E是（i）具有芳基或杂芳基侧链的天然或非天然氨基酸残基或其衍生物; 或（ii）NHR'，其中R'是C 1 -C 24烃基，任选地含有一个或多个选自N，O和S的杂原子，和 任选地包含一个或多个H-键受体或供体部分; 所述烃基还包含侧链C 4 -C 12芳基或杂芳基，其本身可任选被一个或多个选自H-键供体部分 ，H-键受体部分，卤素，Me，Et，Pr，CF 3，CN和NO 2; 其中当A，B，C，D和E各自通过羧酰胺基团与相应的相邻残基连接时，A和E中的至少一个不是天然或非天然氨基酸残基。

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