• Starting from commercially available dioxaspiro decan ol was

  2022-09-06

  

  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 INDY catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was obtai

• In addition to their functional activation of GPR

  2022-09-06

  

  In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic Folinic acid synthesis to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner,

• br Materials animals and methods

  2022-09-03

  

  Materials, animals and methods Results Discussion This study presents mice with a missense point mutation in R258 of FFAR1 that has functional consequences. Firstly, in islets of Ffar1R258W/R258W mice, both the physiological agonist palmitate and the synthetic agonist TUG-469 were unable to

• Free fatty acid receptor FFAR also known as GPR

  2022-09-03

  

  Free fatty risedronic acid sale receptor 1 (FFAR1, also known as GPR40) belongs to the family of G protein-coupled receptors (GPCRs) and was de-orphanized in 2003 as a receptor for medium-to long-chain free fatty acids (FFAs) [9,10]. Mainly expressed in beta cells of pancreatic islets, GPR40 can be

• br Methods GLUT DS was diagnosed either when

  2022-09-03

  

  Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF Bilirubin below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percentile and CSF

• Limitations of our study are the following we

  2022-09-03

  

  Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we

• With the exception of R none of the other

  2022-09-03

  

  With the exception of R5.40310, none of the other residues would appear to be in a position to mediate direct agonist interactions in the active state GLP-1R structures. ECL2 within the GLP-1R is important for affinity and efficacy of both extended and processed GLP-1 peptides [24]. Though distal fr

• Recently unimolecular multi functional peptides that combine

  2022-09-03

  

  Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with nmda receptor and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and wei

• Gap junctions mediate electrical coupling

  2022-09-03

  

  Gap junctions mediate electrical coupling between cells by conducting direct ionic currents and thereby modulate their electrical activity (Hormuzdi et al., 2004). In the nervous system, electrical coupling organizes network activity by amplifying and synchronizing neuronal firing (Galarreta and He

• Our own search towards aryl imidazole derived GSMs led to

  2022-09-03

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• br FXR expression in normal intestine and cancer Of note

  2022-09-03

  

  FXR LCL161 in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al., 2013, Kemper et al., 2009,

• br ACKNOWLEDGMENTS br Introduction Odorant receptors ORs are

  2022-09-03

  

  ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed a

• We characterized the enzyme corresponding to N FPP was the

  2022-09-03

  

  We characterized the enzyme corresponding to N1. FPP was the most effective substrate as allylic diphosphate, and the activities with GPP and DMAPP were 50% and 11% that with FPP, respectively. The analysis of the prenols resulting from the treatment of prenyl diphosphates with Go 6983 receptor pho

• The ETA receptor has a higher affinity for

  2022-09-03

  

  The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec

• The molecular mechanisms underlying VSMC ETB receptor upregu

  2022-09-03

  

  The molecular mechanisms underlying VSMC ETB receptor upregulation have been studied after 24–48h organ culture in both coronary and cerebral arteries. The increased expression of contractile ETB receptor at these time points has been shown to depend on transcriptional mechanisms and PKC and the ext

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