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Classical DHFR inhibitors such as methotrexate MTX
2019-08-02
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Lapatinib residues as well as hydrophobic
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SIRT has deacetylated regulation on numerous nonhistone prot
2019-08-01
SIRT1 has deacetylated regulation on numerous nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016) to play a key role in protecting against cell stress. Therefore, the role of SIRT1 in fluorine-induced oxidative stress was explored. The results reveal
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Enterobacteriaceae are gram negative rods that include the
2019-08-01
Enterobacteriaceae are gram negative rods that include the Escherichia coli and Shigella. There are several DNA ligases posted on the GenBank belong mostly to Enterobacteria phages, such as the T4 bacteriophage [30]. There are several protein markers used to differentiate between T4 phage superfamil
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The only reported synthesis of the
2019-08-01
The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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br Conclusion Our objective is to promote cell activity on
2019-08-01
Conclusion Our objective is to promote cell activity on biomaterials, especially for use in regenerative medicine, by grafting THPs containing collagen-binding sites onto inert substrates. We have previously reported a methodology to derivatize EDC/NHS crosslinked films with photoreactive THPs. T
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TNF a major cytokine that is
2019-08-01
TNF-α, a major cytokine that is critical in acute and chronic inflammation, is responsible from chemotaxis, acute phase reactions and endothelial activation (Mahalingam and Karupiah, 1999). Our study showed that TNF-α is increased significantly in the pyelonephritic rats and montelukast displayed an
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Bisindolylmaleimide IV br Material and methods br Results br
2019-08-01
Material and methods Results Discussion Conclusions To conclude, although CPT2 and CPT1 must have co-evolved to establish the carnitine shuttling, these enzymes are the most distantly related carnitine transferases, split early in evolution, during which a switch occurred in their locati
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br Estrogen receptors activate mGluR signaling pathways In
2019-08-01
Estrogen receptors activate mGluR signaling pathways In order to distinguish the opposing effects of estradiol on CREB phosphorylation, we turned to a “bottom-up” approach, working backwards from CREB phosphorylation to pharmacologically isolate the two signaling pathways (Boulware et al., 2005).
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In the horse oviduct the EP receptor
2019-08-01
In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial Purvalanol B is particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely reflects diffe
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Thus RhoA mediated inhibition of DGK
2019-08-01
Thus RhoA-mediated inhibition of DGKθ is a well-characterized pathway, conserved from C. elegans to mammalian tissues, which enables G-protein coupled receptors to regulate the extent and kinetics of DAG-mediated signaling by fine tuning DGK enzymatic activity. Acknowledgments Introduction Ce
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br Substrate characterization of candidate peptide
2019-07-31
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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In addition to vasoconstrictor actions acute
2019-07-31
In addition to vasoconstrictor actions (acute effects), ET-1 exerts potent mitogenic actions on vascular smooth muscle cells and cardiac myocytes (chronic effects), hence causing vascular and cardiac hypertrophy [19,24,25]. These effects are mediated via stimulation of either ETA or ETB receptors, a
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br Conformational Activation of APC C Enables
2019-07-31
Conformational Activation of APC/C Enables Binding to the Coactivator CDC20 APC/C comes to life by binding a coactivator. This is controlled in part by phosphorylation and APC/C conformational changes that expose the S1RA for the C box and IR tail of the coactivator. In interphase when mitotic ki
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br Materials and Methods br
2019-07-31
Materials and Methods Acknowledgements We thank the staff of beamlines ID29 and ID30A-1 of the European Synchrotron Radiation Facility. This work was supported by, the Marie Curie Career Integration Grant (PCIG13-GA-2013-630755), the Israel Science Foundation (Grant 1383/17) and the Israeli Ca
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The mesolimbic dopamine system is believed to be
2019-07-31
The mesolimbic dopamine system is believed to be highly important for evaluating environmental stimuli in order to generate an adaptive behavioral response. Thus, not surprisingly these functions appear to have been highly conserved across the vertebrate subphylum. Even though teleost fish lack midb
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