专利号:WO-9624694-A1 优先权日:1995-02-10 标 题:Method and kit for fluorometric analysis of enzymes catalyzing synthesis of nucleic acids 发明人:CHAVAN SURENDRA J; PROCHASKA HANS J 权利人:SLOAN KETTERING INST CANCER 摘要:This invention provides a method for detecting in a sample an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. Also provided is a method for determining in a sample the activity of such an enzyme. This invention also provides a method for detecting an RNA-DNA heteroduplex in a sample which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. This method for detecting an RNA-DNA heteroduplex may further comprise quantitatively determining detected RNA-DNA heteroduplex. This invention also provides a method for detecting in a sample en enzyme which catalyzes the synthesis of and RNA-DNA heteroduplex from a nucleic acid template, as well as a method of detecting the activity of such an enzyme in a sample. This invention further provides a method for detecting the viral load of HIV in a sample. Also provided is a method for diagnosing an HIV infection in a subject, and for monitoring the progression of an HIV infection in a subject. Also provided is a method for determining the viral load of HIV in a subject infected with HIV. This invention further provides a method for identifying whether a substance inhibits reverse transcriptase. Finally, this invention provides a kit for assaying an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template.
专利号:US-2004053355-A1 优先权日:2000-05-26 标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors 发明人:WAINER IRVING; MARKOGLOU NEKTARIA 摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.
专利号:US-2006177929-A1 优先权日:2003-03-24 标题 :Regulation of self-renewal in stem cells 发明人:KLUG CHRISTOPHER A 权利人:KLUG CHRISTOPHER A 摘要:Disclosed are methods for regulating the self-renewal capacity of stem cells such as, but not limited to, primitive hematopoietic stem cells (HSCs) (both mouse and human) by modulating the function and/or activity of target factors that are controlled or altered in their regulation by AML1-ETO expression in stem cells such as HSC. Target factors include, but are not limited to, AML1, C/EBP alpha, and/or PU.1 either individually, or in combinations, Altering the function and/or activity of such target factors in HSC leads to inhibition of HSC differentiation and stimulation of HSC self-renewal capacity. Modulation of target factor activity may be achieved at the level of synthesis of these target factors, interaction with cellular factors required for basal activity or enhanced activity, such as cofactors, interactions with their DNA binding motifs, or by targeted degradation or inhibition of their mRNAs.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-7838053-B2 优先权日:2004-03-11 标题:Barley for production of flavor-stable beverage 发明人:BREDDAM KLAUS; OLSEN OLE; SKADHAUGE BIRGITTE; LOK FINN; KNUDSEN SOEREN; BECH LENE MOELSKOV 权利人:CARLSBERG AS 摘要:According to the invention, there is provided null-LOX-1 barley and plant products produced thereof, such as malt manufactured by using barley kernels defective in synthesis of the fatty acid-converting enzyme lipoxygenase-1. Said enzyme accounts for the principal activity related to conversion of linoleic acid into 9-hydroperoxy octadecadienoic acid, a lipoxygenase pathway metabolite, which-through further enzymatic or spontaneous reactions-may lead to the appearance of trans-2-nonenal. The invention enables brewers to produce a beer devoid of detectable trans-2-nonenal-specific off flavors, even after prolonged storage of the beverage.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
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