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    • 22. 发明授权
    • Method of identifying a useful set of signal transduction proteins from a multiplicity of potentially useful proteins
    • 从多种潜在有用的蛋白质中鉴定有用的一组信号转导蛋白的方法
    • US07504230B2
    • 2009-03-17
    • US10714163
    • 2003-11-13
    • Lawrence M. Kauvar
    • Lawrence M. Kauvar
    • G01N33/53
    • G01N33/5014Y10T436/12
    • The present invention is a cell-based method of identifying a set of signal transduction proteins having an intracellular localization pattern responsive to toxic compounds. The method requires identifying and screening an initial set of signal transduction proteins against a set of toxic compounds, and determining changes in intracellular localization pattern of each of the proteins. Proteins whose changes in intracellular localization pattern are redundant are discarded from the initial set, and new proteins are added to provide a new set of proteins. I repeat the method steps with new sets of proteins until the set of proteins provides me at least 5 principal components with respect to the range of compounds marketed as small organic molecules.
    • 本发明是鉴定具有对有毒化合物有响应的细胞内定位模式的一组信号转导蛋白的基于细胞的方法。 该方法需要鉴定和筛选针对一组有毒化合物的初始信号转导蛋白,并确定每种蛋白质的细胞内定位模式的变化。 蛋白质的细胞内定位模式的变化是冗余的,从初始集合中被丢弃,并添加新的蛋白质以提供一组新的蛋白质。 我重复使用新的蛋白质组的方法步骤,直到蛋白质集合相对于作为小有机分子销售的化合物的范围至少提供了5个主要成分。
    • 25. 发明授权
    • Real time detection of intermolecular interaction
    • 实时检测分子间相互作用
    • US07238490B2
    • 2007-07-03
    • US11187336
    • 2005-07-21
    • Lawrence M. Kauvar
    • Lawrence M. Kauvar
    • G01N33/53
    • C40B30/04G01N33/566G01N33/6845G01N33/6857
    • Intermolecular binding can be detected by formation of a “paratope” which results in an immediate generation of a signal. The substances to be tested for interaction are bound to demitopes, wherein said demitopes are components of a paratope which binds a reporter which provides said signal when bound. Known interactions measured in this way can also be employed to screen for compounds which interfere with the interactions. In addition to testing for individual interactions, the interaction of a compound with a library or library×library interactions can also be determined and the effect of potentially interfering substances evaluated.
    • 分子间结合可以通过形成导致立即产生信号的“同位素”来检测。 待测试的相互作用的物质与分子结合,其中所述分子是与结合时提供所述信号的报告物结合的对位基团的组分。 以这种方式测量的已知相互作用也可用于筛选干扰相互作用的化合物。 除了测试个体相互作用之外,还可以确定化合物与文库或文库相互作用的相互作用,并评估潜在的干扰物质的影响。
    • 27. 发明授权
    • Urethane mediated, GST specific molecular release systems
    • 氨基甲酸酯介导的GST特异性分子释放系统
    • US5908919A
    • 1999-06-01
    • US476119
    • 1995-06-07
    • Lawrence M. KauvarMatthew H. LyttleApparao Satyam
    • Lawrence M. KauvarMatthew H. LyttleApparao Satyam
    • A61K38/00A61K38/04A61P35/00C07K5/02C07K5/023C07K5/037C07K5/08A61K38/06
    • C07K5/0215A61K38/00
    • Compounds of the formula ##STR1## or of the formula ##STR2## or the amides, esters or salts thereof, wherein: S.sup.x is S.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.3 wherein R.sup.3 is alkyl (1-6C) or O--C.dbd.O or HN--C.dbd.O;each R of R.sup.1, and R.sup.2 is independently H or a noninterfering substituent;wherein (conj) represents a conjugated system capable of transmitting electrons;n is 0 or 1;YCO is selected from the group consisting of .gamma.-Glu, .gamma.-Glu-Gly, Glu, Glu-Gly, .beta.Asp, .beta.-Asp-Gly, Asp and Asp-Gly;AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of Formula 1; andN(Z) represents a reduced nitrogen-containing leaving group and L represents an electron-withdrawing leaving group,are useful as prodrugs and to generate active components released by the activity of glutathione S-transferase.
    • 式或式的化合物或其酰胺,酯或盐,其中:Sx为S = O,O = S = O,S = NH,HN = S = O,Se = O,O = Se = O ,Se = NH,HN = Se = O,S + R3,其中R3是烷基(1-6C)或OC = O或HN-C = O; R 1的每个R和R 2独立地为H或非干扰取代基; 其中(conj)表示能够传输电子的共轭系统; n为0或1; YCO选自γ-Glu,γ-Glu-Gly,Glu,Glu-Gly,β-Asp,β-Asp-Gly,Asp和Asp-Gly; AAC是通过肽键与所述式1化合物的剩余部分连接的氨基酸; 并且N(Z)表示还原的含氮离去基团,L表示吸电子离去基团,可用作前药并产生通过谷胱甘肽S-转移酶活性释放的活性成分。
    • 30. 发明授权
    • Method for analyte classification by SC profiles
    • SC剖面分析方法
    • US5674688A
    • 1997-10-07
    • US129413
    • 1993-09-29
    • Lawrence M. KauvarStuart M. Ambler
    • Lawrence M. KauvarStuart M. Ambler
    • G01N30/02G01N33/53G01N33/543G01N33/566G06F17/30
    • G01N33/53G01N30/02Y10S435/975Y10S436/808Y10S436/815Y10S436/816Y10S436/817Y10S436/901
    • The precision of identification of analyte composition in a sample, where the possible analytes each provide a series of values for characteristic parameters; in particular where the parameters are generated by cross-reaction with specific binding reagents, is enhanced by applying pattern recognition techniques. Samples to be tested are evaluated with respect to each survey parameter to obtain a pattern of parameter values with respect to each analyte at a given concentration. In the case of the use of a panel of specific binding reagents, the samples to be tested are reacted with this panel and the affinities at various analyte concentrations are determined. This results in a databank of "SC profiles" for known concentrations of each analyte. This databank is stored in a computationally accessible form, which then can be matched against SC profiles obtained by testing unknown samples.
    • 样品中分析物组成的鉴定精度,其中可能的分析物各自提供一系列特征参数值; 特别是通过与特异性结合试剂进行交叉反应产生参数时,通过应用模式识别技术得到增强。 针对每个测量参数评估要测试的样品,以获得相对于给定浓度的每种分析物的参数值的模式。 在使用一组特异性结合试剂的情况下,待测试样品与该面板反应,并确定各种分析物浓度下的亲和力。 这导致每个分析物的已知浓度的“SC概况”的数据库。 该数据库以计算可访问的形式存储,然后可以与通过测试未知样本获得的SC简档进行匹配。