• Because of its excellent GPR

  2022-04-12

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Relevance was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel

• G protein coupled receptor GPCR ligands can be classified

  2022-04-12

  

  G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa

• Glycine regulates several brain functions

  2022-04-12

  

  Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter

• The existence of EAAT subtypes raises

  2022-04-12

  

  The existence of 5 EAAT subtypes raises obvious questions as to the cellular and anatomical distribution of the various transporters (for review, see Gegelashvili & Schousboe, 1998, Danbolt, 2001). While difference in techniques (i.e., protein vs. mRNA), reagents, and preparations (i.e., in vivo vs.

• Finally it is possible that the increase in the number

  2022-04-12

  

  Finally, it is possible that the increase in the number of EAAT-3-labelled cells in the DG at PD 60, when compared with the control and experimental animals at PD 14, is associated with natural changes in the number of neurons present during the postnatal development of the hippocampus (41, 42) and,

• Epidemiological evidence indicates that neuroinflammation pl

  2022-04-12

  

  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

• Epidemiological studies revealed that vitamin D deficiency w

  2022-04-12

  

  Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio

• Expression and translocation of GLUT are

  2022-04-12

  

  Expression and translocation of GLUT4 are regulated by various mechanisms including protein kinase C isoforms (PKCs) and mitogen-activated protein kinase (MAPK) signals [22], [23], but the real mechanism that statins alter expression and function of GLUT4 has not been fully identified. It is general

• br Results br Discussion ER

  2022-04-12

  

  Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in

• br Results and Discussion br STAR Methods br Author

  2022-04-12

  

  Results and Discussion STAR★Methods Author Contributions Conflicts of Interest J.P.F. is a consultant for AstraZeneca, BMS, Johnson and Johnson, Novo Nordisk, and Sanofi, a member of the advisory panel for AstraZeneca and Sanofi, a member of the speaker’s bureau for Sanofi and Novo Nordi

• GLP and glucose dependent insulinotropic peptide GIP

  2022-04-12

  

  GLP-1 and glucose-dependent insulinotropic peptide (GIP) are gut hormones secreted from intestinal L NP118809 mg and K cells, respectively. Together, these hormones account for the vast majority of the incretin effect, the enhanced postprandial insulin secretion observed in healthy adults (Dupre et 

• Besides its established insulinotropic actions GIP has

  2022-04-12

  

  Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M

• br Materials and methods br Results

  2022-04-12

  

  Materials and methods Results Discussion BTB, as a necessary structure for the spermatogenic epithelium, provides an important internal environmental for spermatogenesis and its disruption leads to male infertility (Qiu et al., 2016). GJs and TJs which are mainly components of BTB play esse

• Some aspects of intercellular Ca wave spread are similar to

  2022-04-12

  

  Some aspects of intercellular Ca2+ wave spread are similar to the phenomenon of spreading depression and associated with migraine headache [57]. These depolarization waves, followed by electrical inhibition, are evoked by transient hypoxia and other types of Toremifene injury and spread slowly acros

• dpni AD is an irreversible and

  2022-04-12

  

  AD is an irreversible and progressive neurodegenerative disease affecting the dpni which insidiously destroys memory, thinking skills and cognition. Originally described in 1906 by German physician Alois Alzheimer, AD is characterized by the presence of intraneuronal neurofibrillary tangles of hyper

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