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Till date several predictive models have been
2020-06-17
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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br Molecular modeling simulation study Molecular modeling st
2020-06-17
Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the
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br Phylogenetic analysis KSTDs have
2020-06-17
Phylogenetic analysis — Δ1-KSTDs have rather diverse amino prazosin hcl sequences. A sequence distance analysis using the program MEGA6 [75] of all currently biochemically characterized Δ1-KSTDs yielded a largest p-distance [76] of 0.67 (on a scale of 0-1) for the Δ1-KSTDs from the actinobacteria
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In this study we have developed and investigated three NADPH
2020-06-17
In this study we have developed and investigated three NADPH-regenerating fusion partners with two different enzyme systems: a BVMO and an ADH. With the exception of one fusion construct (StGDH with LbADH), all fusion salbutamol sulfate receptor resulted in good soluble expression as well as fully f
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There exists a glucose residue in the structure of Acid
2020-06-17
There exists a glucose residue in the structure of 5. Acid hydrolysis (Supplementary data) followed by TLC comparison with the reference compound as well as GC–MS analysis (l-cysteine methyl ester hydrochloride derivative: tR=22.22min for glucose residue of 5 and 22.46min for the reference compound)
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br O GlcNAc transferase OGT belongs
2020-06-17
O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t
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br Acknowledgements We would like to thank Dr Ron
2020-06-17
Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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br Mechanisms of acquired resistance to st and
2020-06-17
Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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Interestingly global EGFR depletion increased the rate of
2020-06-17
Interestingly, global EGFR depletion increased the rate of cell elimination everywhere in the notum (Figures 2B–2D), irrespective of the deformation status of the cells. Accordingly, we found that recombinant insulin are not any more sensitive to stretching upon EGFR depletion (Figures S6A–S6C; Vide
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Introduction Neuropathic pain occurs in approximately one th
2020-06-17
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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In conclusion we designed novel E inhibitors
2020-06-17
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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RLS is a genetically complex disorder in
2020-06-17
RLS is a genetically complex disorder in which genetic and environmental factors contribute to the phenotype (Trenkwalder, Allen, Högl, Paulus, & Winkelmann, 2016). This disease is highly familial and six genetic variants with single nucleotide polymorphisms have been identified by genome-wide assoc
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br Material and methods br Discussion First
2020-06-16
Material and methods Discussion First, we investigated cannabis use, and results showed that the lifetime prevalence of cannabis use in our sample was 29.63%, with a significant difference between males (73.8% of the abusers) and females (26.2%). Moreover, the mean age and age at onset were si
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Ultrasound is an acoustic wave with a frequency kHz that
2020-06-16
Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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kinase inhibitor In view of the hypotensive effect
2020-06-16
In view of the hypotensive effect of endothelial-specific overexpression of eNOS [17], [19], [28] we correlated skeletal muscle eNOS expression with sBP including data on colony 5 of eNOS-Tg [17] which was used to generate eNOS-Tg/KO (Fig. 4D). We found a highly significant one phase exponential dec
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