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    Fluorogenic substrates for .beta.-lactamase and methods of use
    21.
    发明授权
    Fluorogenic substrates for .beta.-lactamase and methods of use 失效
    β-内酰胺酶的荧光底物和使用方法

    公开(公告)号：US5741657A

    公开(公告)日：1998-04-21

    申请号：US407544

    申请日：1995-03-20

    申请人： Roger Y. Tsien ,  Gregor Zlokarnik

    发明人： Roger Y. Tsien ,  Gregor Zlokarnik

    IPC分类号： C12N15/09 ,  C07D463/00 ,  C07D471/04 ,  C07D501/00 ,  C07D501/20 ,  C07D501/59 ,  C07D505/00 ,  C12N5/02 ,  C12N5/10 ,  C12N9/86 ,  C12N15/55 ,  C12N15/85 ,  C12P17/18 ,  C12P35/00 ,  C12Q1/34 ,  C12Q1/68 ,  C07D501/14

    CPC分类号： C07D501/36 ,  C07D501/00 ,  C07D505/00 ,  C07D519/00 ,  C12N15/85 ,  C12N9/86 ,  C12P17/184 ,  C12P17/188 ,  C12P35/00 ,  C12Q1/18 ,  C12Q1/34 ,  C12Q1/6897 ,  C12N2800/90 ,  C12N2830/002 ,  C12Q2334/00 ,  G01N2333/986 ,  G01N2415/00 ,  Y10S435/805

    摘要： Fluorogenic substrates of the general formula I ##STR1## in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R' is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH.sub.2 OH).sub.n OH, in which n is 0 or an integer from 1 to 5; R" is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, --CHR.sup.2 OCO(CH.sub.2).sub.n CH.sub.3, --CHR.sup.2 OCOC(CH.sub.3).sub.3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R.sup.2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO.sub.2 and CH.sub.2 ; and Z' and Z" are linkers for the fluorescent donor and quencher moieties. The substrates are useful in conjunction with .beta.-lactamase as reporter gene in a wide range of assays, for example to determine protein localization or bacterial resistance.

    摘要翻译： 其中X和Y中的一个是荧光供体部分，另一个是淬灭剂（其可以或不再发射）的通式I 的荧光底物; R'选自H，低级（即1至约5个碳原子的烷基）和（CH 2 OH）nOH，其中n为0或1至5的整数; R“选自H，生理学上可接受的金属和铵阳离子，-CHR2OCO（CH2）nCH3，-CHR2OCOC（CH3）3，酰基硫代甲基，酰氧基-α-苄基，δ-丁基内酰基，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基 ，β-吗啉代乙基，二烷基氨基乙基，酰氧基烷基，二烷基氨基羰氧基甲基和脂族基，其中R2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z'和Z“是荧光供体和猝灭剂部分的接头。 在广泛的测定中，底物可与β内酰胺酶作为报告基因结合使用，例如确定蛋白质定位或细菌耐药性。

    PHOTON REDUCING AGENTS FOR FLUORESCENCE ASSAYS
    23.
    发明申请
    PHOTON REDUCING AGENTS FOR FLUORESCENCE ASSAYS 有权
    用于荧光测定的光子还原剂

    公开(公告)号：US20130004960A1

    公开(公告)日：2013-01-03

    申请号：US13437846

    申请日：2012-04-02

    申请人： Tom KNAPP ,  Gregor Zlokarnik ,  Paul Negulesou ,  Roger Y. Tsien ,  Timothy James Rink

    发明人： Tom KNAPP ,  Gregor Zlokarnik ,  Paul Negulesou ,  Roger Y. Tsien ,  Timothy James Rink

    IPC分类号： G01N21/64 ,  G01N21/75

    CPC分类号： G01N33/582 ,  C12Q1/682 ,  G01N33/5005 ,  G01N33/542 ,  Y10S436/80 ,  Y10S436/809 ,  Y10T436/13 ,  C12Q2563/107 ,  C12Q2527/125

    摘要： The present invention provides a method for reducing undesirable light emission from a sample using at least one photon producing agent and at least one photon reducing agent (e.g. dye-based photon reducing agents). The present invention further provides a method for reducing undesirable light emission from a sample (e.g., a biochemical or cellular sample) with at least one photon producing agent and at least one collisional quencher. The present invention also provides a method for reducing undesirable light emission from a sample (e.g., a biochemical or cellular sample) with at least one photon producing agent and at least one quencher, such as an electronic quencher. The present invention also provides a system and method of screening test chemicals in fluorescent assays using photon reducing agents. The present invention also provides compositions, pharmaceutical compositions, and kits for practicing these methods.

    摘要翻译： 本发明提供一种使用至少一种光子产生剂和至少一种光子还原剂（例如基于染料的光子还原剂）来减少来自样品的不希望的光发射的方法。 本发明进一步提供了用至少一种光子产生剂和至少一种碰撞猝灭剂减少来自样品（例如生物化学或细胞样品）的不希望的光发射的方法。 本发明还提供了用至少一种光子产生剂和至少一种猝灭剂（例如电子猝灭剂）减少来自样品（例如，生物化学或细胞样品）的不希望的光发射的方法。 本发明还提供了使用光子还原剂在荧光测定中筛选测试化学品的系统和方法。 本发明还提供了用于实施这些方法的组合物，药物组合物和试剂盒。

    Substrates for β-lactamase and uses thereof
    26.
    发明授权
    Substrates for β-lactamase and uses thereof 有权
    β-内酰胺酶底物及其用途

    公开(公告)号：US07157575B2

    公开(公告)日：2007-01-02

    申请号：US10280482

    申请日：2002-10-24

    申请人： Roger Y. Tsien ,  Gregor Zlokarnik

    发明人： Roger Y. Tsien ,  Gregor Zlokarnik

    IPC分类号： C07D501/14

    CPC分类号： C07D501/36 ,  C07D501/00 ,  C07D505/00 ,  C07D519/00 ,  C12N9/86 ,  C12N15/85 ,  C12N2800/90 ,  C12N2830/002 ,  C12P17/184 ,  C12P17/188 ,  C12P35/00 ,  C12Q1/18 ,  C12Q1/34 ,  C12Q1/6897 ,  C12Q2334/00 ,  G01N2333/986 ,  G01N2415/00 ,  Y10S435/805

    摘要： Substrates for β-lactamase of the general formula I in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R′ is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R″ is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z′ and Z″ are linkers for the fluorescent donor and quencher moieties. Methods of assaying β-lactamase activity and monitoring expression in systems using β-lactamase as a reporter gene also are disclosed.

    摘要翻译： 通式I的β-内酰胺酶底物，其中X和Y中的一个是荧光供体部分，另一个是猝灭剂（其可以或不再发射）; R'选自H，低级（即1至约5个碳原子的烷基）和（CH 2 CH 2）n OH，其中n是 0或1〜5的整数; R“选自H，生理学上可接受的金属和铵阳离子，-CHR 2 OCO（CH 2）n CH 酰基硫基甲基，酰氧基-α-苄基，三氟甲磺酸酯，三氟甲磺酸酯， 丁基内酰胺，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基，酰氧基烷基，二烷基氨基羰氧基甲基和脂族基，其中R 2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z'和Z“是荧光供体和猝灭剂部分的接头。 公开了使用β-内酰胺酶作为报道基因的体内测定β-内酰胺酶活性和监​​测表达的方法。

    Use of inhibitors in reporter assays
    28.
    发明授权
    Use of inhibitors in reporter assays 失效
    在报道测定中使用抑制剂

    公开(公告)号：US06284461B1

    公开(公告)日：2001-09-04

    申请号：US09067612

    申请日：1998-04-28

    申请人： Gregor Zlokarnik ,  Luxin Feng

    发明人： Gregor Zlokarnik ,  Luxin Feng

    IPC分类号： C12Q168

    CPC分类号： C12Q1/34 ,  G01N2333/986

    摘要： The present invention relates to methods for increasing the signal-to-noise ratio of an enzyme assay by contacting a sample comprising a membrane compartment with an inhibitor of an enzyme, contacting the sample with a substrate for the enzyme, and determining the activity of the enzyme. The method can be in a heterogeneous or homogeneous format. The methods of the present invention can be used for a variety of purposes, such as increasing the dynamic range of an enzyme assay, extending the useful loading time or assay measurement time of an enzyme assay, profiling the level of an enzyme in a sample, modulating the threshold activity of an enzyme assay, screening test compounds for activity, identifying modulators, identifying an inhibitor of an enzyme, and detecting membrane permeability. The present invention also relates to compounds useful in these methods.

    摘要翻译： 本发明涉及通过使包含膜隔室的样品与酶的抑制剂接触来提高酶测定的信噪比的方法，使样品与酶的底物接触，并测定其活性 酶。 该方法可以是异构或均匀的格式。 本发明的方法可以用于各种目的，例如增加酶测定的动态范围，延长酶测定的有用加载时间或测定时间，分析样品中酶的水平， 调节酶测定的阈值活性，筛选测试化合物的活性，鉴定调节剂，鉴定酶的抑制剂，以及检测膜渗透性。 本发明还涉及可用于这些方法的化合物。

    Substrates for .beta.-lactamase and uses thereof
    29.
    发明授权
    Substrates for .beta.-lactamase and uses thereof 失效
    β-内酰胺酶底物及其用途

    公开(公告)号：US5955604A

    公开(公告)日：1999-09-21

    申请号：US955401

    申请日：1997-10-21

    申请人： Roger Y. Tsien ,  Gregor Zlokarnik

    发明人： Roger Y. Tsien ,  Gregor Zlokarnik

    IPC分类号： C07D501/00 ,  C07D501/14 ,  C12Q1/34

    CPC分类号： C07D501/00 ,  C09B11/24 ,  C09B15/00 ,  C09B19/00 ,  C09B23/04 ,  C09B23/08 ,  C09B23/145 ,  C09B47/24 ,  C09B57/02 ,  C09B57/08 ,  Y10S435/805

    摘要： Substrates for .beta.-lactamase of the general formula I ##STR1## in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R' is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH.sub.2).sub.n OH, in which n is 0 or an integer from 1 to 5; R" is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, --CHR.sup.2 OCO(CH.sub.2).sub.n CH.sub.3, --CHR.sup.2 OCOC(CH.sub.3).sub.3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R.sup.2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO.sub.2 and CH.sub.2 ; and Z' and Z" are linkers for the fluorescent donor and quencher moieties. Methods of assaying .beta.-lactamase activity and monitoring expression in systems using .beta.-lactamase as a reporter gene also are disclosed.

    摘要翻译： 通式I的β-内酰胺酶底物，其中X和Y中的一个是荧光供体部分，另一个是猝灭剂（其可以或不再发射）; R'选自H，低级（即1至约5个碳原子的烷基）和（CH 2）nOH，其中n为0或1至5的整数; R“选自H，生理学上可接受的金属和铵阳离子，-CHR2OCO（CH2）nCH3，-CHR2OCOC（CH3）3，酰基硫代甲基，酰氧基-α-苄基，δ-丁基内酰基，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基 ，β-吗啉代乙基，二烷基氨基乙基，酰氧基烷基，二烷基氨基羰氧基甲基和脂族基，其中R2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z'和Z“是荧光供体和猝灭剂部分的接头。 公开了使用β-内酰胺酶作为报告基因的系统中测定β-内酰胺酶活性和监​​测表达的方法。