Enzyme inhibitory

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  • "Bioactive Food Peptides in Health and Disease" highlights recent developments on bioactive food peptides for the promotion of human health and the prevention/management of chronic diseases. The book provides a comprehensive revision of bioactive peptides obtained from both animal and plant food sources. Aspects related to their bioactivity, mechanism of action, and bioavailability are extensively described along the different chapters.

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  • THE EXTENT AND TIMING OF PLANT GROWTH are controlled by the coordinated actions of positive and negative regulators. Some of the most obvious examples of regulated nongrowth are seed and bud dormancy, adaptive features that delay growth until environmental conditions are favorable. For many years, plant physiologists suspected that the phenomena of seed and bud dormancy were caused by inhibitory compounds, and they attempted to extract and isolate such compounds from a variety of plant tissues, especially dormant buds.

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  • We have previously reported that sulfoquinovosylmonoacylglycerol (SQMG) is a potent inhibitor of mammalian DNA polymerases. DNA polymeraseb(pol b) is one of the most important enzymes protecting the cell against DNA damage by base excision repair. In this study, we charac-terized the inhibitory action of SQMG against rat pol b. SQMG competed with both the substrate and the template-primer for binding to polb.

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  • Amino-(3,4-dihydroxyphenyl)methyl phosphonic acid, the phosphonic analogof 3,4-dihydroxyphenylglycine, hadbeen previously reported as a potent inhibitor of tyrosinase. The mechanism of the apparent enzyme inhibition by this com-pound has now been established. Amino-(3,4-dihydroxy-phenyl)methyl phosphonic acid turned out to be a substrate and was oxidized too-quinone, which evolved to a final product identified as 3,4-dihydroxybenzaldehyde, the same as for 3,4-dihydroxyphenylglycine.

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  • The study and therapeutic modulation of purinergic signaling is hindered by a lack of specific inhibitors for NTP diphosphohydrolases (NTPDases), which are the terminating enzymes for these processes. In addition, little is known of the NTPDase protein structural elements that affect enzymatic activity and which could be used as targets for inhibitor design.

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  • Other Diseases The power and versatility of gene transfer approaches are such that there are few serious disease entities for which gene transfer therapies are not under development. Besides those already discussed, other areas of interest include gene therapies for HIV and for neurodegenerative disorders.

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  • The protein arginine methyltransferase (PRMT) family of enzymes cata-lyzes the transfer of methyl groups from S-adenosylmethionine to the gua-nidino nitrogen atom of peptidylarginine to form monomethylarginine or dimethylarginine. We created several less polar analogs of the specific PRMT inhibitor arginine methylation inhibitor-1, and one such compound was found to have improved PRMT inhibitory activity over the parent molecule.

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  • Highly active, small-molecule furin inhibitors are attractive drug candidates to fend off bacterial exotoxins and viral infection. Based on the 22-residue, active Lys fragment of the mung bean trypsin inhibitor, a series of furin inhibitors were designed and synthesized, and their inhibitory activity towards furin and kexin was evaluated using enzyme kinetic analysis.

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  • HIV-1 protease is an important target for treatment of AIDS, and efficient drugs have been developed. However, the resistance and negative side effects of the current drugs has necessitated the development of new compounds with different binding patterns. In this study, nine C-terminally duplicated HIV-1 protease inhibitors were cocrystallised with the enzyme, the crystal structures analysed at 1.8–2.3 A˚ resolution, and the inhibitory activity of the compounds characterized inorder toevaluate the effects of the individual modifications. ...

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