• In summary we have designed and optimized a

  2022-03-11

  

  In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr

• The treatment target which aims

  2022-03-11

  

  The “90-90-90 treatment target” which aims at diagnosing 90% of HIV-infected individuals, treating 90% of those diagnosed and achieve viral suppression for 90% of treated individuals, is a key strategy to achieve one of the sustainable development goals (SDG) of ending AIDS as a public health threat

• GnRH ant have been designed to obtain pharmacological compou

  2022-03-11

  

  GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p

• The calculations for the R substrate showed that like the

  2022-03-11

  

  The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn annexin v is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchanged roles

• Through a large scale phylogenetic analysis of

  2022-03-11

  

  Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 ddr1 can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in eubacteria gen

• BCCA occlusion followed by reperfusion injury significantly

  2022-03-11

  

  BCCA occlusion, followed by reperfusion injury, significantly increased the brain AT1 and AT2 receptor expression in mice. Reports have demonstrated elevation of AT1 receptor expression in the cerebral Solamargine during ischemia [34,35]. The gene expression of brain AT2 receptor is increased in bot

• br Discussion The Pro Ala variant in PPARG has

  2022-03-11

  

  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

• Epidemiological evidence indicates that neuroinflammation pl

  2022-03-11

  

  Epidemiological evidence indicates that neuroinflammation plays a pivotal role in pathogenesis of AD (Heneka et al., 2015, Heneka et al., 2013, Holmes et al., 2009, Liu et al., 2016). For example, prolonged treatment with nonsteroidal anti-inflammatory drugs reduces the risk of developing AD (In et

• In this study we present the synthesis and structure

  2022-03-11

  

  In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g

• Axons are the largest component

  2022-03-11

  

  Axons are the largest component of WM by volume and are a significant repository of intracellular glutamate that can be releases under ischemic conditions [1,3,4,29,117]. We have recently shown that the principle route by which mature myelinated BAMB-4 release glutamate during acute ischemia is via

• br Conclusions The results of this work showed

  2022-03-11

  

  Conclusions The results of this work showed that β-glucosidase could be efficiently immobilized onto hydroxyapatite nanoparticles in a single adsorption step. The enzyme adsorption was accomplished by coordination bonds between remaining Ca2+ sites of HA and COO− of amino acids. The immobilizatio

• The findings in this study may represent an example of

  2022-03-10

  

  The findings in this study may represent an example of a more general phenomenon, namely that the exquisite specificity of the G protein-coupled receptors that mediate the physiological actions of the Spectinomycin hydrochloride hydrate synthesis family hormones in mammals may have arisen relativel

• br Financial support This work was

  2022-03-10

  

  Financial support This work was supported by Fondation pour la Recherche Médicale (Equipe labellisée, DEQ20150331724), Inserm, University of Lille, and Agence Nationale pour la Recherche (ANR-10-LBEX-46 and ANR-10-INBS-08; ProFI project, “Infrastructures Nationales en Biologie et Santé”; “Investi

• Vincristine receptor br Results and discussion The synthesis

  2022-03-10

  

  Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou

• br Acknowledgements br Introduction Pregnancy

  2022-03-10

  

  Acknowledgements Introduction Pregnancy brings forth significant metabolic reprogramming that induces a number of metabolic changes to ensure that the nutrient requirements of the mother and fetus are met [[1], [2], [3]]. These adaptations change radically over the period of pregnancy dependin

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