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W J Greenlee E D Thorsett J P Springer A A Patchett E H Ulm T C Vassil 《Biochemical and biophysical research communications》1984,122(2):791-797
A class of potent inhibitors of angiotensin-converting enzyme (dipeptidyl carboxypeptidase, E.C. 3.4.15.1) is reported, in which an alpha-aza substitution into the substituted N-carboxymethyl dipeptide structure of enalapril is made. The inhibitors 2 exhibit striking alterations in their conformational and acid-base properties due to the aza substitution, as is clear from pKa data and the x-ray crystal structure of a model azapeptide. In spite of this, they bind tightly to the enzyme, with inhibitor potency comparable to that of captopril. 相似文献
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Semko CM Chen L Dressen DB Dreyer ML Dunn W Farouz FS Freedman SB Holsztynska EJ Jefferies M Konradi AW Liao A Lugar J Mutter L Pleiss MA Quinn KP Thompson T Thorsett ED Vandevert C Xu YZ Yednock TA 《Bioorganic & medicinal chemistry letters》2011,21(6):1741-1743
A series of N-(pyrimidin-4-yl)-phenylalanine VLA-4 antagonists is described. Optimization of substituents at the 2 and 5 positions of the pyrimidine ring gave 14, a very potent VLA-4 inhibitor which is orally active in a sheep asthma model. 相似文献
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Pehun Pereyra Gerber Lidia M. Duncan Edward JD Greenwood Sara Marelli Adi Naamati Ana Teixeira-Silva Thomas WM Crozier Ildar Gabaev Jun R. Zhan Thomas E. Mulroney Emily C. Horner Rainer Doffinger Anne E. Willis James ED Thaventhiran Anna V. Protasio Nicholas J. Matheson 《PLoS pathogens》2022,18(2)
Efforts to define serological correlates of protection against COVID-19 have been hampered by the lack of a simple, scalable, standardised assay for SARS-CoV-2 infection and antibody neutralisation. Plaque assays remain the gold standard, but are impractical for high-throughput screening. In this study, we show that expression of viral proteases may be used to quantitate infected cells. Our assays exploit the cleavage of specific oligopeptide linkers, leading to the activation of cell-based optical biosensors. First, we characterise these biosensors using recombinant SARS-CoV-2 proteases. Next, we confirm their ability to detect viral protease expression during replication of authentic virus. Finally, we generate reporter cells stably expressing an optimised luciferase-based biosensor, enabling viral infection to be measured within 24 h in a 96- or 384-well plate format, including variants of concern. We have therefore developed a luminescent SARS-CoV-2 reporter cell line, and demonstrated its utility for the relative quantitation of infectious virus and titration of neutralising antibodies. 相似文献
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Joann?Mudge Steven?B?Cannon Peter?Kalo Giles?ED?Oldroyd Bruce?A?Roe Christopher?D?Town Nevin?D?YoungEmail author 《BMC plant biology》2005,5(1):15
Background
Recent genome sequencing enables mega-base scale comparisons between related genomes. Comparisons between animals, plants, fungi, and bacteria demonstrate extensive synteny tempered by rearrangements. Within the legume plant family, glimpses of synteny have also been observed. Characterizing syntenic relationships in legumes is important in transferring knowledge from model legumes to crops that are important sources of protein, fixed nitrogen, and health-promoting compounds. 相似文献18.
ANDRÉ SCHUITEMAN JAAP JAN VERMEULEN ED DE VOGEL ART VOGEL 《Botanical journal of the Linnean Society. Linnean Society of London》2011,167(3):344-350
Bulbophyllum nocturnum , a species of section Epicrianthes from New Britain, is described and illustrated. It is the first known example of an orchid species in which the flowers open after dark and close in the morning. The poorly understood pollination biology of section Epicrianthes, a clade with highly unusual flowers, is discussed. Attention is drawn to the close resemblance between the petal appendages of some species and the fruiting bodies of certain Myxogastria. © 2011 The Linnean Society of London, Botanical Journal of the Linnean Society, 2011, 167 , 344–350. 相似文献
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The physiological capacity for sucrose breakdown in developingjuice sac cells of acid limes was estimated by assaying theactivity of the three enzymes of sucrose catabolism in additionto vacuolar acid hydrolysis. The maximum potential rates ofsucrose breakdown were compared with the observed rates of carbonutilization. Highest potential rates of sucrose breakdown (28.621mmol cm3 per hydrated active space d1) occurredat the initial stages of fruit development where carbon utilizationwas highest. As the fruit developed, the potential rates ofsucrose breakdown and carbon utilization declined to very lowlevels. At 80% of development, vacuolar acid hydrolysis becamethe only physiological mechanism for sucrose breakdown. Therelatively low amounts of sucrose hydrolysed by acid hydrolysisat this time were just sufficient to account for the measuredcarbon demands. The results suggest that carbon supplied bythis distinct sucrose catabolizing system is able to provideadequate levels of carbon skeletons for the observed levelsof respiration and dry weight deposition early in development,but becomes a limiting factor for growth in the later stages. Key words: Vacuolar acid hydrolysis, Citrus aurantifolia 相似文献