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The structural similarity software vROCS
2021-12-10

The structural similarity software vROCS (OpenEye) [45] has been utilized by Musumeci et al. [46] to screen the Maybridge [47] HitFinder database (∼14,400 compounds) using Distamycin A (Fig. 3B) as a query. Using the Tanimoto coefficient (Section 6.4) and vROCS's colour scoring (atom/feature similar
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Preliminary explorations focused on the linker of
2021-12-10

Preliminary explorations focused on the linker of 2 (Table 1). Lilly reported that the methylene between the phenyl and the piperidyl group was metabolically susceptible to N-dealkylation, so we replaced the methylene with a carbonyl moiety to block the metabolic site [23,48] (Fig. 2). In addition,
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br Author contributions br Acknowledgements The
2021-12-10

Author contributions Acknowledgements The work was supported in part by Natural Science Foundation of China (31601995, 31501028) and an internal research grant of Jianghan University (14042). The authors thank HY of Jingchu University of technology for revising the manuscript. Introduction
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We tested this hypothesis with two experiments In the first
2021-12-09

We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 enkephalin (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemically mimicking
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The aim of this study is to explore new
2021-12-09

The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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Carbetocin The need for an inflammatory risk
2021-12-09

The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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br Regulation of Glu transporters The pivotal
2021-12-09

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino nisin synthesis calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include tran
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EAATs can transport glutamate aspartate cysteic
2021-12-09

EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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MicroRNA or miRNA is group of RNA molecule of about
2021-12-09

MicroRNA, or miRNA, is group of RNA molecule of about 22 nucleotides without protein-coding function. MicroRNAs are widely distributed in plants, animals and even some viruses and participant in both normal physiological and pathological processes by post-transcriptional regulation of gene expressio
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Although the ramifications of non additive SAR are context
2021-12-09

Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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Cx mimetic peptides short synthetic peptides corresponding
2021-12-09

Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino 2-APB sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concentrati
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In the upper part of the intestine a
2021-12-09

In the upper part of the intestine a small amount of conjugated BAs are reabsorbed via passive diffusion, whereas the part of BAs that escape enterohepatic circulation passes into the colon where they undergo bacterial conversions such as deconjugation, dehydroxylation or dehydrogenation, into secon
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PK profiles of were evaluated and
2021-12-09

PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 cell
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Therefore the histomorphology and the comprehensive analysis
2021-12-09

Therefore, the histomorphology and the comprehensive analysis of TMJ-RA pathogenesis need to be completed although clinical findings in TMJ-RA are similar to RA in other joints [41]. Especially for the dentist, the difficulties associated with diagnosing TMJ-RA patients [49] posing challenges to dia
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The product chain length determination mechanism of
2021-12-09

The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino AMG-458 sale residues in each subfamily of -prenyltransferases have enabled the understanding of the basic catal
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