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Esomeprazole Sodium Introduction Enzymes have higher selecti
2019-11-25

Introduction Enzymes have higher selectivity, specificity and efficiency than chemical catalysts. Due to their properties and their green chemistry, biocatalysts are widely used in food, textile and pharmaceutical industry [1], [2]. A high efficient biocatalyst for industrial applications must be s
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br Conclusion The past few years have witnessed
2019-11-25

Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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A variety of fused membered
2019-11-25

A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG
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This review focuses on the atomic basis
2019-11-25

This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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Sex has been shown to mediate the relationship between
2019-11-25

Sex has been shown to mediate the relationship between allelic differences in COMT and behavior (Harrison & Tunbridge, 2008). The COMT promoter region contains 2 estrogen response elements (Xie, Ho, & Ramsden, 1999) that can inhibit the formation of COMT (Jiang, Xie, Ramsden, & Ho, 2003). With regar
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SPR was used to measure biomolecular kinetic interactions
2019-11-25

SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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Nevertheless because of the preclinical
2019-11-25

Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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In summary we have identified a series
2019-11-25

In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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Based upon these findings on portions A
2019-11-25

Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for
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Gliptins have become a part
2019-11-22

Gliptins have become a part of various therapeutic regimens to treat type 2 diabetics in recent decades. Gliptins were developed to lower the blood glucose in type 2 diabetes patients and have been shown to be effective [4,5]. More than a dozen gliptins have been developed for the treatment of T2DM,
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In this contribution herein we report our newly devised
2019-11-22

In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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Traditionally serum triglycerides have been measured in the
2019-11-22

Traditionally, serum triglycerides have been measured in the clinic in the fasted state in order to reduce variability and also to facilitate the calculation of LDL-cholesterol via the Friedewald equation, which was derived using fasted samples (Warnick and Nakajima, 2008). We have previously report
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In summary these findings show that
2019-11-22

In summary, these findings show that the knockdown of tra2 in the Drosophila fat body results in an increased triglyceride phenotype, which could be explained in part by altered splicing of the gene coding for the lipid breakdown enzyme, CPT1. These findings are consistent with previous studies anal
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Indeed some studies that examined the morphine response have
2019-11-22

Indeed, some studies that examined the morphine response have reported that the (C) allele of rs4818 was associated with a low dose administered compared to that given for individuals with the (G) allele (Rakvag et al., 2008). In a publication about Tunisian patients with cancer by Chatti et al. (2
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br Materials and methods br Results
2019-11-22

Materials and methods Results Recombinant, N-terminally His6-tagged vCPH was purified to near homogeneity via a modification of the reported procedure and its identity confirmed by intact protein mass spectrometry (Supplementary Fig. 1). As reported, vCPH catalysed two hydroxylations of a PAPK
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