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Susmitha Valli Gogula Ch Divakar Ch Satyanarayana Yedla Phani Kumar Vadapalli Santhosi Lavanaya 《Bioinformation》2013,9(20):1040-1043
Diabetic Retinopathy (DR) is one of the attenuating complications of diabetes mellitus. The key gene responsible for causing
diabetic retinopathy is protein kinase C beta (PKCβ). Protein kinase C is a family of protein kinase enzymes which are involved in
controlling the function of other proteins through phosphorylation mechanism and plays a crucial role in signal transduction
mechanisms. Among all the PKC isoenzymes, PKCβ could be a significant isoenzyme involved in vascular dysfunction during
hyperglycemia. Studies show that oral administration of PKCβ inhibitor Ruboxistaurin (), decreases vessel permeability
and improves retinal condition. Thus compounds that decrease the PKCβ activation would be helpful in the treatment of diabetic
retinopathy. The compounds similar to Ruboxistaurin are taken from Super Target database and docking analysis was performed.
Maleimide derivative 3 showed highest binding affinities compared to Ruboxistaurin and so we advise that compound may be
utilized in the treatment of diabetic retinopathy. LY333531相似文献
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Exploration of the function and organization of the yeast early secretory pathway through an epistatic miniarray profile 总被引:23,自引:0,他引:23
Schuldiner M Collins SR Thompson NJ Denic V Bhamidipati A Punna T Ihmels J Andrews B Boone C Greenblatt JF Weissman JS Krogan NJ 《Cell》2005,123(3):507-519
We present a strategy for generating and analyzing comprehensive genetic-interaction maps, termed E-MAPs (epistatic miniarray profiles), comprising quantitative measures of aggravating or alleviating interactions between gene pairs. Crucial to the interpretation of E-MAPs is their high-density nature made possible by focusing on logically connected gene subsets and including essential genes. Described here is the analysis of an E-MAP of genes acting in the yeast early secretory pathway. Hierarchical clustering, together with novel analytical strategies and experimental verification, revealed or clarified the role of many proteins involved in extensively studied processes such as sphingolipid metabolism and retention of HDEL proteins. At a broader level, analysis of the E-MAP delineated pathway organization and components of physical complexes and illustrated the interconnection between the various secretory processes. Extension of this strategy to other logically connected gene subsets in yeast and higher eukaryotes should provide critical insights into the functional/organizational principles of biological systems. 相似文献
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ER-associated degradation (ERAD) of glycoproteins depends on dual recognition of protein misfolding and remodeling of the substrate's N-linked glycans. After recognition, substrates are retrotranslocated to the cytosol for proteasomal degradation. To explore the directionality of this process, we fused a highly stable protein, DHFR, to the N or C terminus of the soluble ERAD substrate CPY* in yeast. Degradation of the C-terminal CPY*-DHFR fusion is markedly slowed and is accompanied by DHFR release in the ER lumen. Thus, folded lumenal domains can impede protein retrotranslocation. The ER lumenal protein Yos9p is required for both release of DHFR and degradation of multiple ERAD substrates. Yos9p forms a complex with substrates and has a sugar binding pocket that is essential for its ERAD function. Nonetheless, substrate recognition persists even when the sugar binding site is mutated or CPY* is unglycosylated. These and other considerations suggest that Yos9p plays a critical role in the bipartite recognition of terminally misfolded glycoproteins. 相似文献
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Wittig olefination of 5,6-dideoxy-5,6-anhydro-6-nitro-d-glucofuranose (5) triggered a concomitant cyclisation via oxy Michael addition of the C2-hydroxyl group resulting in the formation of C-vinyl glycosides with Z-olefinic geometry. 相似文献
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Christopher R. McCullough Phani Kumar Pullela Sang-Choul Im Lucy Waskell Daniel S. Sem 《Journal of biomolecular NMR》2009,43(3):171-178
The cytochromes P450 (CYPs) play a central role in many biologically important oxidation reactions, including the metabolism
of drugs and other xenobiotic compounds. Because they are often assayed as both drug targets and anti-targets, any tools that
provide: (a) confirmation of active site binding and (b) structural data, would be of great utility, especially if data could
be obtained in reasonably high throughput. To this end, we have developed an analog of the promiscuous heme ligand, cyanide,
with a 13CH3-reporter attached. This 13C-methyl isocyanide ligand binds to bacterial (P450cam) and membrane-bound mammalian (CYP2B4) CYPs. It can be used in a rapid
1D experiment to identify binders, and provides a qualitative measure of structural changes in the active site.
Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users. 相似文献