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The typical pharmacophore for GPR agonists contains four par
2021-10-07

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Thus from this preliminary study a working model of HIV
2021-10-07

Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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br Discussion The LISA analysis indicated
2021-10-07

Discussion The LISA analysis indicated that HIV was geographically clustered in the north-west districts of Amhara Region. A high rate of HIV infection was found in Metema and Mirab Armacho districts, which share borders with Eretria and Sudan. Various studies have linked risk of infectious disea
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br Methods The study was
2021-10-07

Methods The study was a cross-sectional, ecological analysis of country-reported HIV expenditures. We obtained the most recent available and validated data on annual country-reported HIV expenditures in SSA countries between 2012 and 2017 from the UNAIDS (http://aidsinfo.unaids.org/). Many countr
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The lower number of samples tested for
2021-10-07

The lower number of samples tested for the comparison between cobas 4800 HIV-1 and RealTime HIV-1, especially at or below 50 copies/mL (Table 6), could limit our ability to discern a difference in the ability of the various assays to identify patients with virological failure. However, the 95% CI ar
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At the present time there are several clinical trial studies
2021-10-07

At the present time, there are several clinical trial studies being conducted with a variety of indications for pitolisant. Various studies in different phases assess different aspects of pitolisant efficacy and safety in narcoleptic patients (Szakacs et al., 2017) (NCT01800045, NCT02611687, NCT0343
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Reactivation of memory engram neurons underlies memory retri
2021-10-07

Reactivation of memory engram neurons underlies memory retrieval. Neurons activated during memory formation are reactivated during the memory test 24, 25, 32. The reactivation is observed in the cerebral cortex as well as in the hippocampus and amygdala 33, 34. The ratio of the reactivation correlat
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Of the many thousands of mutations analyzed in tracheal term
2021-10-07

Of the many thousands of mutations analyzed in tracheal terminal cells, less than a handful affect tube morphology specifically in the transition zone (Baer et al., 2007, Beitel and Krasnow, 2000, Förster et al., 2010, Ghabrial et al., 2011, Myat et al., 2005, Ruiz et al., 2012, Samakovlis et al., 1
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EdU is a thymidine analog that is incorporated into replicat
2021-10-07

EdU is a thymidine analog that is incorporated into replicated chromosomal DNA during the S phase of the cell cycle. DAPI is a fluorescent dye that binds strongly to A-T-rich regions in DNA and is commonly used for cell nucleus staining. We used the EdU incorporation assay, which is a highly sensiti
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The different NO stimulated and ODQ inhibited cNMP patterns
2021-10-07

The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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br Materials and methods br Results br Discussion
2021-10-07

Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin 2478 and functionally characterized the majority of the receptors wh
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Starting from commercially available dioxaspiro decan ol
2021-10-07

Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an BAMB-4 catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was obtain
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lomitapide br Materials and methods br
2021-10-06

Materials and methods Results Discussion Defective regulation and inappropriate activation of the HH signaling pathway is implicated in many cancers. SMO targeting inhibitors were the first to enter clinical trials, however complications with acquired resistance and toxicity, also exemplifi
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Recently a lot of synthetic FFA agonists containing acidic
2021-10-04

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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Corresponding to the different insulinotropic signaling the
2021-10-04

Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Arecaidine but-2-ynyl ester tosylate on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric b
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