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A remodelled protease that cleaves phosphotyrosine substrates 总被引:1,自引:0,他引:1
Knight ZA Garrison JL Chan K King DS Shokat KM 《Journal of the American Chemical Society》2007,129(38):11672-11673
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n.O.e. difference spectra reveal that the preferred solution conformation of methyl enol ethers has the methyl group -periplanar to the double bond; n.O.e kinetics in a methoxy—heptatriene demonstrate the presence of both possible periplanar conformations, the energy difference being 1 kcal/mole. 相似文献
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The reversible phosphorylation of proteins is one of the most important mechanisms for the regulation of signal transduction cascades. Recently, there has been substantial progress made in the identification of new phosphoproteins and phosphorylation sites. Unfortunately, there are very few methods available that allow this information to be used to identify the upstream kinase responsible for the phosphorylation event. Herein, we describe a new method that allows the cross-linking of a substrate of interest to its upstream kinase. This method relies upon a novel, mechanism-based cross-linker and the replacement of the phosphorylated residue with a cysteine residue. The application of this method to a number of kinase-peptide substrate pairs is described. 相似文献
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The cancer drug, Imatinib, is a selective Abl kinase inhibitor that does not inhibit the closely related kinase c-Src. This one drug and its ability to selectively inhibit Abl over c-Src has been a guiding principle in virtually all kinase drug discovery efforts in the last 15 years. A prominent hypothesis explaining the selectivity of Imatinib is that Abl has an intrinsic ability to adopt an inactive conformation (termed DFG-out), whereas c-Src appears to pay a high intrinsic energetic penalty for adopting this conformation, effectively excluding Imatinib from its ATP pocket. This explanation of the difference in binding affinity of Imatinib for Abl versus c-Src makes the striking prediction that it would not be possible to design an inhibitor that binds to the DFG-out conformation of c-Src with high affinity. We report the discovery of a series of such inhibitors. We use structure-activity relationships and X-ray crystallography to confirm our findings. These studies suggest that small molecules are capable of inducing the generally unfavorable DFG-out conformation in c-Src. Structural comparison between c-Src in complex with these inhibitors allows us to speculate on the differential selectivity of Imatinib for c-Src and Abl. 相似文献
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A host-guest optical sensor for the determination of aliphatic amines as exemplified by octylamine is proposed. It is based
on the reversible fluorescence enhancement of heptakis(2,6-di-O-isobutyl)-β-cyclodextrin(DOB-β-CD) hosting tetraphenylporphyrin
(TPP) immobilized in poly(vinyl chloride) (PVC) membrane by aliphatic amine extracted from aqueous phase into membrane phase.
The optimum membrane contained 1.15 wt % TPP, 6.15 wt % DOB-β-CD as sensing reagent and other membrane materials. The fluorescence
enhancement of the membrane resulted from the formation of a stable three-component complex among DOB-β-CD, TPP, and aliphatic
amines. With the optimum conditions described, the fluorescence response of the sensor to octylamine shows a good correlation
with the theoretically derived equation in the range 1.0 × 10–6 to 8.0 × 10–4 mol/L. The response characteristics including reversibility, response time, reproducibility and lifetime and selectivity
of this optical device are also discussed in detail. This sensor has also been applied for the determination of octylamine
in water samples containing interferents with satisfactory recovery.
Received: 21 November 1999 / Revised: 10 January 2000 / Accepted: 15 January 2000 相似文献