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91.
V.?P.?ShevchenkoEmail author I.?Yu.?Nagaev Yu.?V.?Kuznetsov E.?V.?Polunin A.?A.?Zozulya N.?F.?Myasoedov 《Russian Journal of Bioorganic Chemistry》2005,31(4):378-382
A synthesis of olanzapine, 2-methyl-10-(4-methyl-1-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine, was carried out and the conditions for its tritium labeling were optimized to obtain a tritium-labeled olanzapine preparation with a specific radioactivity of 12 Ci/mmol.__________Translated from Bioorganicheskaya Khimiya, Vol. 31, No. 4, 2005, pp. 420–424.Original Russian Text Copyright © 2005 by Shevchenko, Nagaev, Kuznetsov, Polunin, Zozulya, Myasoedov. 相似文献
92.
OI Klychnikov AV Drabkin OV Vasilenko YS Pavlov MS Trofimova IN Smolenskaya AA Rozenkranz AS Sobolev AV Babakov 《Biochemistry. Biokhimii?a》1998,63(9):1083-1089
Higher plant plasma membranes carry receptors of different affinity for the phytotoxin fusicoccin. Reception of fusicoccin involves proteins belonging to the highly conserved 14-3-3 family, but the complete structure of the fusicoccin receptor (FCR) is unknown. Using radiation inactivation analysis, we estimated the molecular masses of low-affinity and high-affinity FCR at 63 +/- 7 and 130 +/- 15 kD, respectively. The dose dependences of receptor inactivation indicate that microsomal specimens contain "silent" FCRs of 420 +/- 90 kD in amounts commensurate with that of the active FCRs. Both low- and high-affinity FCRs are inactivated by hydrolytic enzymes from the outer surface of the plasma membrane, and impairment of protoplast integrity causes an irreversible transition of the low-affinity binding site into the high-affinity one. A scheme is proposed for the organization of different types of FCR in the plasma membrane, implying that the membrane affinity for fusicoccin reflects the interaction between proteins in the FCR complex. 相似文献
93.
NaCl-preferring NZB/B1NJ mice and NaCl-avoiding CBA/J mice have similar amiloride inhibition of chorda tympani responses to NaCl 总被引:1,自引:1,他引:0
Integrated chorda tympani nerve responses to NaCl were studied in two mouse
strains, an NaCl-preferring NZB/B1NJ and an NaCl-avoiding CBA/J. The NaCl
responses of both strains had similar magnitude and were suppressed by
amiloride to a similar extent. This suggests that peripheral gustatory
responsiveness to NaCl is not the only mechanism underlying mouse strain
variation in NaCl acceptance.
相似文献
94.
Petro Borysko Yurii S. Moroz Oleksandr V. Vasylchenko Vasyl V. Hurmach Anastasia Starodubtseva Natalia Stefanishena Kateryna Nesteruk Sergey Zozulya Ivan S. Kondratov Oleksandr O. Grygorenko 《Bioorganic & medicinal chemistry》2018,26(12):3399-3405
A combination approach of a fragment screening and “SAR by catalog” was used for the discovery of bromodomain-containing protein 4 (BRD4) inhibitors. Initial screening of 3695-fragment library against bromodomain 1 of BRD4 using thermal shift assay (TSA), followed by initial hit validation, resulted in 73 fragment hits, which were used to construct a follow-up library selected from available screening collection. Additionally, analogs of inactive fragments, as well as a set of randomly selected compounds were also prepared (3?×?3200 compounds in total). Screening of the resulting sets using TSA, followed by re-testing at several concentrations, counter-screen, and TR-FRET assay resulted in 18 confirmed hits. Compounds derived from the initial fragment set showed better hit rate as compared to the other two sets. Finally, building dose-response curves revealed three compounds with IC50?=?1.9–7.4?μM. For these compounds, binding sites and conformations in the BRD4 (4UYD) have been determined by docking. 相似文献
95.
NOBORU FUJINAMI YUKITAKA SUGIMOTO ATSUYOSHI HAGIWAAA 《Development, growth & differentiation》1973,15(2):141-151
Enhancement of the erythroid maturation in Friend virus-induced leukemic cells has been examined in vitro by the treatment with dimethyl sulfoxide (DMSO). Although the cell growth was inhibited in the medium containing 2% DMSO, many cells remained viable for a week. By the 3rd day of the culture, the cells treated with DMSO became more strongly agglutinated by phytohemagglutinin than the cells incubated without DMSO. Mouse erythrocyte membrane-specific antigens were also detectable at the 4th day. At the 8th day of the culture hemoglobin synthesis was apparently demonstrated in the cells treated with DMSO, which could not be seen in the untreated cells. Maturation or differentiation along the erythroid pathway in Friend leukemic cells by DMSO is discussed on these markers. 相似文献
96.
We have developed a digital image processing technique based on highpass filtering of microfluorimetric images for selective transmission of fine image details corresponding to mitochondria. This technique enabled the detection of the mitochondrial calcium signals with high selectivity, simultaneously with the cytosolic calcium signal. The validity of this technique was supported in primary cultures of rat brain capillary endothelial cells loaded with X-rhod-1 by the results that (i) inhibition of the mitochondrial Ca2+ uptake by discharging the mitochondrial membrane potential selectively abolished the transient of the highpass filtered signal evoked by ATP, and (ii) CGP-37157, a selective blocker of the mitochondrial Na+/Ca2+ exchanger, increased the peak amplitude of highpass filtered (mitochondrial) Ca2+ transients and caused a sustained plateau. The highpass filtering technique enabled the analysis of the mitochondrial Ca2+ transients in high temporal resolution. We found a uniform and monophasic rise of [Ca2+] in the mitochondrial population of the cell, following the cytosolic [Ca2+] with a delay at onset and peak. The introduced highpass filtering technique is a powerful tool in the high spatial and temporal resolution analysis of mitochondrial calcium transients, and it could be especially important in specimens where genetically targeted probes fail. 相似文献
97.
V. M. Kavsan V. V. Dmitrenko K. O. Shostak T. V. Bukreieva N. Y. Vitak O. E. Simirenko T. A. Malisheva M. I. Shamayev V. D. Rozumenko Y. A. Zozulya 《Cytology and Genetics》2007,41(1):30-48
To enhance glioblastoma (GB) marker discovery, we compared gene expression in GB with human normal brain (NB) by accessing
the SAGE Genie web site and compared the results with published data. Nine GB and five NB SAGE libraries were analyzed using
the Digital Gene Expression Displayer (DGED); the results of DGED were tested by Northern blot analysis and RT-PCR of arbitrarily
selected genes. Review of available data from the articles on gene expression profiling by microarray-based hybridization
showed as few as 35 overlapped genes with increased expression in GB. Some of them were identified in four articles, but most
genes were identified in three or even in two investigations. Some differences were also found between SAGE results of GB
analysis. The Digital Gene Expression Displayer approach revealed 676 genes differentially expressed in GB vs. NB with cutoff
ratio: twofold change and P ≤ 05. Differential expression of selected genes obtained by DGED was confirmed by Northern analysis
and RT-PCR. Altogether, only 105 of 955 genes presented in published investigations were among the genes obtained by DGED.
Comparison of the results obtained by microarrays and SAGE is very complicated because the authors present only the most prominent
differentially expressed genes. However, even available data give quite poor overlapping of genes revealed by microarrays.
Some differences between results obtained by SAGE in different investigations can be explained by high dependence on the statistical
methods used. As for now, the best solution to search for molecular tumor markers is to compare all available results and
to select only those genes where significant expression in tumors combined with very low expression in normal tissues was
reproduced in several articles. One hundred five differentially expressed genes, common to both methods, can be included in
the list of candidates for the molecular typing of GBs. Some genes, encoded cell surface or extracellular proteins may be
useful for targeting gliomas with antibody-based therapy.
The text was submitted by the authors in English. 相似文献
98.
Curves of transitions in double (2-->1 transition) and triple (3-->2 transition) complexes of oligonucleotides dA(N1)with dT(N2) in solutions with Na(+) and Mg(2+) are calculated for the case of oligomer lengths from 10 to 500 nucleotides in the wide range of ion concentrations. The calculated curves of transitions and their differential analogs reflect rather exactly the position and form of experimental curves and describe dependences of transition temperatures on the length of molecules, their concentration, and ionic conditions. Values of the nucleation parameter beta for the systems studied are determined by comparison of the calculated and experimental data obtained in a number of works. The average beta value equal to 10(-3) l/mole is in an agreement with values reported for similar systems earlier. It is shown that disordering of duplex and triplex ends ("end fraying") has an essential influence on the form of melting curves, their asymmetry and the increase of the transition interval. 相似文献
99.
The impact of glia-derived extracellular matrices on the barrier function of cerebral endothelial cells: an in vitro study 总被引:4,自引:0,他引:4
The blood-brain barrier (BBB) is composed of the cerebral microvascular endothelium, which, together with astrocytes, pericytes, and the extracellular matrix (ECM), contributes to a "neurovascular unit". It was our objective to clarify the impact of endogenous extracellular matrices on the barrier function of BBB microvascular endothelial cells cultured in vitro. The study was performed in two consecutive steps: (i) The ECM-donating cells (astrocytes, pericytes, endothelial cells) were grown to confluence and then removed from the growth substrate by a protocol that leaves the ECM behind. (ii) Suspensions of cerebral endothelial cells were seeded on the endogenous matrices and barrier formation was followed with time. In order to quantify the tightness of the cell junctions, all experiments were performed on planar gold-film electrodes that can be used to read the electrical resistance of the cell layers as a direct measure for endothelial barrier function (electric cell-substrate impedance sensing, ECIS). We observed that endogenously isolated ECM from both, astrocytes and pericytes, improved the tightness of cerebral endothelial cells significantly compared to ECM that was derived from the endothelial cells themselves as a control. Moreover, when cerebral endothelial cells were grown on extracellular matrices produced by non-brain endothelial cells (aorta), the electrical resistances were markedly reduced. Our observations indicate that glia-derived ECM - as an essential part of the BBB - is required to ensure proper barrier formation of cerebral endothelial cells. 相似文献
100.
David C Crossman Allison C Morton Julian P Gunn John P Greenwood Alistair S Hall Keith AA Fox Andrew J Lucking Marcus D Flather Belinda Lees Claire E Foley 《Trials》2008,9(1):1-14