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br Introduction A great many isoprenoids with
2022-05-26

Introduction A great many isoprenoids with varieties of structural diversity, such as steroids, carotenoids, prenyl quinones, and natural rubber, occur in nature. All of these biosynthetic precursors are constructed by the action of prenyl chain elongating enzymes [1], [2], [3], [4]. These enzyme
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The suboptimal trypsin selectivity profile of DPC
2022-05-26

The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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br Acknowledgments We would like to thank
2022-05-26

Acknowledgments We would like to thank Coordenação de Aperfeiçoamento de Pessoal do Ensino Superior (CAPES) and Conselho Nacional de Desenvolvimento Cientifico e Tecnológico (CNPq) for the grants and scholarships provide to the authors of this work. Introduction Human Immunodeficiency Virus t
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br cAMP cGMP effector systems in
2022-05-25

cAMP/cGMP effector systems in human platelets (PKA, PKG, PDEs) In eukaryotic cells, the effects of intracellular cAMP are mediated by two types of cAMP-dependent protein kinases (PKA type I and II) and cAMP-regulated guanine nucleotide exchange factors (EPAC/cAMP-GEF) which activate the RAS GTPas
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α-mangostin As comparators compounds and were
2022-05-25

As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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Introduction In the s nitric
2022-05-25

Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P
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To apply the recently developed GPR ligands to CNS
2022-05-25

To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the CA-074 and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, the pre
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molarity to grams Ning et al showed that LPC appeared to inc
2022-05-25

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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br Gastrointestinal peptides and intestinal health Gastroint
2022-05-25

Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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Starting from commercially available dioxaspiro
2022-05-25

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 Glutathione (GSH/GSSG/Total) Fluorometric Assay Kit mg catalyzed deprotection efficiently ga
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br Funding M I is supported by
2022-05-25

Funding M.I. is supported by European Research Council (ERC) Consolidator Grant 725038, Italian Association for Cancer Research (AIRC) Grant 19891, Italian Ministry of Health (MoH) Grant GR-2011-02347925, Lombardy Foundation for Biomedical Research (FRRB) Grant 2015-0010, the European Molecular B
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The aims of the present study were
2022-05-25

The aims of the present study were to further investigate the localisation of glycine and GABAA receptors on individual neurons and how closely these two receptor types were associated with each other by carrying out double immunofluorescent labelling and imaged using confocal laser scanning microsc
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It is known that hypercapnia
2022-05-25

It is known that hypercapnia, as well as hypoxia, can result in a decrease in body temperature, but the mechanisms involved are not very well known (Barros and Branco, 1998; Saiki and Mortola, 1996). One 9516 is that when there is an acute hypercapnic exposure, acidosis plays an inhibitory role in
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ICH induced striatal lesion produced
2022-05-25

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino glycosylase transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemi
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endothelin receptor antagonist br Discussion The Pro Ala var
2022-05-25

Discussion The Pro12Ala variant in PPARG has been one of the first candidate SNPs for type 2 diabetes [16], [17]. The rare allele of this variant is associated with a 25% reduced risk for the disease [18]. Given the role of PPARG as both a receptor for NEFA and itself a regulator of fat metabolis
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