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Andriy I. Vovk Lyudmyla A. Kononets Vsevolod Yu. Tanchuk Sergiy O. Cherenok Andriy B. Drapailo Vitaly I. Kalchenko Valery P. Kukhar 《Bioorganic & medicinal chemistry letters》2010,20(2):483-487
Inhibition of Yersinia protein tyrosine phosphatase by calix[4]arene mono-, bis-, and tetrakis(methylenebisphosphonic) acids as well as calix[4]arene and thiacalix[4]arene tetrakis(methylphosphonic) acids have been investigated. The kinetic studies revealed that some compounds in this class are potent competitive inhibitors of Yersinia PTP with inhibition constants in the low micromolar range. The binding modes of macrocyclic phosphonate derivatives in the enzyme active center have been explained using computational docking approach. The results obtained indicate that calix[4]arenes are promising scaffolds for the development of inhibitors of Yersinia PTP. 相似文献
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Sharon Sima Lander Sergiy Chornyy Hazem Safory Amit Gross Herman Wolosker Inna Gaisler‐Salomon 《Genes, Brain & Behavior》2020,19(6)
Glutamate Dehydrogenase 1 (GDH), encoded by the Glud1 gene in rodents, is a mitochondrial enzyme critical for maintaining glutamate homeostasis at the tripartite synapse. Our previous studies indicate that the hippocampus may be particularly vulnerable to GDH deficiency in central nervous system (CNS). Here, we first asked whether mice with a homozygous deletion of Glud1 in CNS (CNS‐Glud1 ?/? mice) express different levels of glutamate in hippocampus, and found elevated glutamate as well as glutamine in dorsal and ventral hippocampus, and increased glutamine in medial prefrontal cortex (mPFC). l ‐serine and d ‐serine, which contribute to glutamate homeostasis and NMDA receptor function, are increased in ventral but not dorsal hippocampus, and in mPFC. Protein expression levels of the GABA synthesis enzyme glutamate decarboxylase (GAD) GAD67 were decreased in the ventral hippocampus as well. Behavioral analysis revealed deficits in visual, spatial and social novelty recognition abilities, which require intact hippocampal‐prefrontal cortex circuitry. Finally, hippocampus‐dependent contextual fear retrieval was deficient in CNS‐Glud1 ?/? mice, and c‐Fos expression (indicative of neuronal activation) in the CA1 pyramidal layer was reduced immediately following this task. These data point to hippocampal subregion‐dependent disruption in glutamate homeostasis and excitatory/inhibitory balance, and to behavioral deficits that support a decline in hippocampal‐prefrontal cortex connectivity. Together with our previous data, these findings also point to different patterns of basal and activity‐induced hippocampal abnormalities in these mice. In sum, GDH contributes to healthy hippocampal and PFC function; disturbed GDH function is relevant to several psychiatric and neurological disorders. 相似文献
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The formation of textures in DNA films with LiCl, NaCl, KCl, RbCl, and CsCl salts has been studied. The films are prepared by evaporation of water solution with highly polymerized calf thymus DNA and excess salt of specific type. For DNA solution with 10 mM concentration of NaCl, KCl, and RbCl the films with dendritic textures have been obtained, whereas in case of CsCl the textures in the films appear only at 30 mM concentration of excess salt in the initial solution. In the solution with LiCl, the textures in DNA films have not been observed within the whole range of concentration of excess salt under consideration. The analysis of parameters of DNA films with different salts has showed that evaporation of solution leads to crystallization of salt ions on DNA macromolecule and formation of DNA‐salt complexes. Electrostatic energy of the system of crystalline ordered ions and charges of DNA chains has been estimated to study the stability of DNA‐salt complexes. The results obtained for different salts have been showed that the presence of DNA macromolecule enhances crystallization as compared with solution without DNA. The property of excess salt to form the crystalline structures has been found to decrease in the following order: KCl > NaCl > RbCl > CsCl > LiCl. The results of estimation are in good agreement with the experimentally observed dependence of texture formation on excess salt type. © 2013 Wiley Periodicals, Inc. Biopolymers 99: 508–516, 2013. 相似文献
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Medinets Sergiy Gasche Rainer Kiese Ralf Rennenberg Heinz Butterbach-Bahl Klaus 《Plant and Soil》2019,445(1-2):335-348
Plant and Soil - Soils are known to be significant sources of atmospheric nitric oxide (NO), a key compound in atmospheric chemistry. NO is a key regulating substance for inter- and intra-species... 相似文献
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Kovalchuk SN Kozhemyako VB Atopkina LN Silchenko AS Avilov SA Kalinin VI Rasskazov VA Aminin DL 《The Journal of steroid biochemistry and molecular biology》2006,101(4-5):226-231
Estrogenic potency of six triterpene glycosides, Holothurin A, Holotoxin A1, Frondoside A, Cucumarioside A2-2 and Cauloside C, that are natural products and semi-synthesized Ginsenoside-Rh2, were examined with yeast two-hybrid system, including expressed genes of human estrogen receptor, hER, the co-activator TIF2 and lacZ as a reporter gene. Only Ginsenoside-Rh2 exhibited significant moderate estrogenic activity in the concentration range of 10−7 to 10−6 M. Its effect was approximately 30% of the activity of 17β-estradiol applied at half-effective concentration. This indicates Ginsenosides-Rh2 is a weak phytoestrogen. The sea cucumber triterpene glycosides, Holothurin A, Holotoxin A1, Cucumarioside A2-2 and Frondoside A, and plant glycoside Cauloside C had no appreciable estrogenic activity. Data obtained by yeast two-hybrid assay reflect structure–activity relationship between tested compounds and 17β-estradiol. Only Ginsenoside-Rh2 has some similarity in chemical structure with 17β-estradiol that might explain affinity of this glycoside to the hER receptor. 相似文献
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Sea Cucumbers Triterpene Glycosides, the Recent Progress in Structural Elucidation and Chemotaxonomy
Vladimir I. Kalinin Alexandra S. Silchenko Sergey A. Avilov Valentin A. Stonik Alexey V. Smirnov 《Phytochemistry Reviews》2005,4(2-3):221-236
Triterpene glycosides are characteristic metabolites of sea cucumbers (Holothurioidea, Echinodermata). Majority of the glycosides
belong to holostane type (lanostane derivatives with 18(20)-lactone). Carbohydrate chains of these glycosides contain xylose,
glucose, quinovose, 3-O-methylglucose and 3-O-methyl sylose. During the last 5 years, main investigations were focused on holothurians belonging to the order Dendrochirotida
collected in the North Pacific, North Atlantic, Antarctic and in subtropical waters. The glycosides of holothurians belonging
to the order Aspidochirotida have also been studied. The most uncommon structural features of carbohydrate chains of new glycosides
were: (1) the presence of quinovose as fifth terminal monosaccharide unit and the presence of two quinovose residues; (2)
the presence of glucose instead of common xylose as fifth terminal monosaccharide unit; (3) trisaccharide carbohydrate chain;
(4) the presence of two 3-O-methylxylose terminal monosaccharide units; (5) the presence of sulfate group at C-3 of quinovose residue. New glycosides
without lactone or with 18(16)-lactone and having shortened side chains have also been isolated. The presence of 17α and 12α-hydroxyls,
which are characteristic for glycosides from holothurians belonging to the family Holothuriidae (Aspidochirotida) in glycosides
of dendrochirotids confirms parallel and relatively independent character of evolution of glycosides. All three families belonging
to the order Aspidochirotida: Holothuriidae, Stichopodidae and Synallactidae have similar and parallel trends in evolution
of the glycosides carbohydrate chains, namely from non-sulfated hexaosides to sulfated tetraosides. Sets of aglycones in glycosides
from holothurians belonging to the genus Cucumaria (Cucumariidae, Dendrochirotida) are specific for each species. The carbohydrate chains are similar in all representatives
of the genus Cucumaria. 相似文献
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High‐Resolution Molecular Validation of Self‐Renewal and Spontaneous Differentiation in Clinical‐Grade Adipose‐Tissue Derived Human Mesenchymal Stem Cells 下载免费PDF全文
Amel Dudakovic Emily Camilleri Scott M. Riester Eric A. Lewallen Sergiy Kvasha Xiaoyue Chen Darcie J. Radel Jarett M. Anderson Asha A. Nair Jared M. Evans Aaron J. Krych Jay Smith David R. Deyle Janet L. Stein Gary S. Stein Hee‐Jeong Im Simon M. Cool Jennifer J. Westendorf Sanjeev Kakar Allan B. Dietz Andre J. van Wijnen 《Journal of cellular biochemistry》2014,115(10):1816-1828
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