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Imidazo purine diones were another cluster of compounds iden
2019-08-13
1-Imidazo[2,1-]purine-2,4(3,8)-diones were another cluster of compounds identified from the Chembridge screen (). A benzyl group at the R2 position was preferred over a phenyl or 2-phenylpropyl (. and ), and -substitution of the benzyl group increased potency to the nanomolar level ( IC=0.20μM . ).
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We recently reported that the information
2019-08-12
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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br Phylogenetic analysis KSTDs have rather
2019-08-12
Phylogenetic analysis — Δ1-KSTDs have rather diverse amino sphingosine 1-phosphate receptor modulator 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
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Only a few studies have examined
2019-08-12
Only a few studies have examined the effect of prostanoids on cardiac fibroblasts. Therefore, this study examines the effect of PGE2 on cardiac fibroblast proliferation and tests the hypothesis that PGE2 causes cardiac fibroblast proliferation via alterations of UNC1999 in regulatory molecules and
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The liposomes as a FDA approved
2019-08-12
The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a
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br Disclosures br Acknowledgements This work was supported
2019-08-12
Disclosures Acknowledgements This work was supported by the Natural Science Foundation of China (No. 81560587); the Fok Ying-Tong Education Foundation of China (No. 151107), the basic ability promotion project for young and middle-aged teachers in Universities in Guangxi (No. 2018KY1146) and t
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Other GPCRs notable for changes in expression on CLL cells
2019-08-12
Other GPCRs notable for changes in expression on CLL cells include upregulation of the thromboxane A2 receptor TBXA2R mRNA [61] and up and downregulation of mRNA and protein from the neurotensin receptors NTSR2 and NTSR1, respectively [62]. The Eμ-TCL1 mouse model of CLL has been used to study mult
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Acidic substituents showed moderate biochemical activity but
2019-08-12
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic ubiquitin e3 ligase were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their bio
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SB 747651A dihydrochloride Besides being an energy storing t
2019-08-12
Besides being an energy storing tissue, adipose tissue acts as an active endocrine organ that secretes a number of biologically active adipokines involved in multiple physiological processes such as inflammation and lipid and glucose metabolism, with direct and indirect effects on reproduction [15,1
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Concerning firmness postharvest calcium dips for whole fruit
2019-08-12
Concerning firmness, postharvest calcium dips for whole fruit have been demonstrated to preserve firmness, cell wall structure (Glenn and Poovaiah, 1990), nutritional quality (Goldberg, 1984) and fruit flavour (Ortiz et al., 2009). Similarly, combinations of calcium treatment (0.5–4%) with packaging
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Soon after the discovery of
2019-08-12
Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).
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Finally the identification of predictive biomarkers of respo
2019-08-09
Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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br Experimental methods br Results and discussion br Conclus
2019-08-09
Experimental methods Results and discussion Conclusions Here we describe the first reported method for high-yield 5-ht receptors of active and soluble mature CPG2 (in the absence of the leader peptide) and its individual catalytic and dimerization domains in E. coli. Such a method is of ke
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lysophosphatidic acid manufacturer br Outcome of COX overexp
2019-08-09
Outcome of COX-2 overexpression Although a causal role for COX-2 has been proposed, mechanisms by which COX-2 function contributes to the pathogenesis of hyperplastic disease are not well defined. To examine if there is any correlation between COX-2 and p53 protein levels, Kumagai et al. [15] rec
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br Conflicts of interest br
2019-08-09
Conflicts of interest Acknowledgements This study was funded by Kuwait University Research Administration (Project MI03/10). Introduction Epidemiological, experimental and biologic plausibility support a cardioprotective effect of estrogens in women [1]. Indeed, women are protected until t
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