• 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

• 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

• 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

• 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

• 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

• 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

• 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

• 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

• 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

• 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

• 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

• 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

• The molecular formula of was assigned as C

  2020-03-31

  

  The molecular formula of 2 was assigned as C12H12N2O2 by the positive HRESIMS at m/z 217.0973 [M+H]+ (calcd for 217.0972), 13C NMR and DEPT spectra, having 8 degrees of unsaturation. The 1H NMR spectrum contains an ABX spin system comprised of resonances at δH 7.47 (d, J=1.9Hz, H-2′), 6.86 (d, J=8.3

• Because of the important role of the DDB

  2020-03-30

  

  Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup

• br Acknowledgments br The design of polyaromatic

  2020-03-30

  

  Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their

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