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Although the implication of DA and
2020-04-01
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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Autoradiography studies have shown cerebellum to be devoid o
2020-04-01
Autoradiography studies have shown NVP-BHG712 to be devoid of D1-R [40], confirming that this region may serve as reference for estimation of free and non-specifically bound radioligand concentration in tissue (= non-displaceable uptake). In initial human studies using [11C]SCH 23390 and [11C]NNC 1
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Bromoenol lactone Many DNA repair pathways are
2020-04-01
Many DNA repair pathways are candidates for DPC repair. Nucleotide excision repair (NER) is widely involved in both bacteria and eukaryotes in removing cross-linked protein with low molecular weights ( recombination (HR) is also involved in some types of DPC (especially >11kDa) (Ide et al., 2011). T
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Molecular modelling studies were performed on the hDHFR inhi
2020-04-01
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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Classical DHFR inhibitors such as methotrexate MTX bind
2020-03-31
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 straight from the source residues as well
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One possible explanation for differences in the
2020-03-31
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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There is an increase in small fruit consumption especially b
2020-03-31
There is an increase in small fruit consumption especially berries in recently. Because small fruits are rich sources of both anthocyanins and phenolic compounds. These chemicals have been found in Vaccinium corymbosum in high levels. Research on small fruits is of vital importance for human nutriti
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Previous study showed that CXCR plays an important role in
2020-03-31
Previous study showed that CXCR plays an important role in viral infection and that CXCR1, as an important molecule in CXCR, also plays important roles in viral pathogenesis [[39], [40], [41], [42]]. In mammals, CXCR1 plays an important role in resisting viral infection [43,44], and CXCR1 plays an i
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br Acknowledgments This work was supported
2020-03-31
Acknowledgments This work was supported by Natural Science Foundation of China (No: 81501485). We are particularly grateful to Dr. Dan Yang and Dr. Yi Zhang for their assistance and facilities in helping this experiment and manuscript. Oral squamous cell carcinoma (OSCC), the most common malig
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Furthermore in silico physicochemical characters and
2020-03-31
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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As a support chitosan presents interesting characteristics t
2020-03-31
As a support, chitosan presents interesting characteristics that reinforce its great potential for enzyme immobilization [18,19]. Firstly, it is produced from renewable natural sources in addition to being biodegradable and water insoluble [20,21]. Also, the main peculiarity in the chitosan structur
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Glycolysis is important to maintain the
2020-03-31
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its acetylcholine receptors metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress
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br Experimental Procedures br Author Contributions br Acknow
2020-03-31
Experimental Procedures Author Contributions Acknowledgments Introduction Oxysterols came to prominence in the late 1970\'s with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on its own synthesis is mediated through oxysterols not by cholesterol itsel
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Based on the above we hypothesized
2020-03-31
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Tacrine amino tetrahydroacridine I Fig was
2020-03-31
Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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