• Molecular properties as well as metabolic stability in

  2022-07-16

  

  Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further

• Given that we planned to isolate the

  2022-07-16

  

  Given that we planned to isolate the GluN1/GluN3A receptor by immunoaffinity chromatography using a Myc epitope tag on GluN3A, we first checked that the tag does not affect the functional properties of the receptor. To do this we co-transfected HEK-293 cells with DNA encoding WT GluN1 and either WT

• Free fatty acid receptor FFAR also known as GPR

  2022-07-16

  

  Free fatty Emodin receptor 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 acti

• Therefore we investigated the acute and delayed

  2022-07-16

  

  Therefore, we investigated the acute and delayed response of 92 human mono- and dizygous twins to an acute shift from low fat to high fat diet with respect to serum levels of VEGF and the expression of SLC2A1 in subcutaneous adipose tissue (AT). By comparing the degree of concordance of basal and di

• There are also data showing potential beneficial effects of

  2022-07-16

  

  There are also data showing potential beneficial effects of SGLT2i on non-alcoholic fatty liver disease (NAFLD) [[14], [15], [16], [17]], a hepatic manifestation of the metabolic syndrome that has been linked to type 2 diabetes mellitus (T2DM) development and increased cardiovascular (CV) as well as

• In this present study the

  2022-07-16

  

  In this present study, the availability of commercial GLUT and SGLT URMC-099 directed against different epitopes, enabled us to screen for members of the SGLT family and compare the expression patterns of GLUTs and SGLTs in the different regions of the rat lens. Based on these regional and subcellu

• Multiple mechanisms have been suggested by which glucagon ca

  2022-07-16

  

  Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met

• br Discussion According to the generally accepted

  2022-07-16

  

  Discussion According to the generally accepted notion which originated from the study of ATP-depleted bepridil the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and the subsequent entry of Ca2+ th

• Interestingly GAL has also been

  2022-07-16

  

  Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion

• Knock out mice of FXR

  2022-07-16

  

  Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon

• br Lung cancer cell lines

  2022-07-16

  

  Lung cancer cell lines The greatest expression of both human and rodent FFA4 transcript has been shown to be localized to the lung [61], yet the physiological role in this tissue has been understudied, as has its involvement in lung cancers. In 2015, a two-staged genome-wide association study of

• br Acknowledgments This research was

  2022-07-16

  

  Acknowledgments This research was supported in part by National Institutes of Health IDeA Program COBRE grant GM110732; a USDA National Institute of Food and Agriculture Hatch project; and the Montana State University Agricultural Experiment Station. Introduction Propofol (2,6-Diisopropylphen

• SM-164 Compounds were tested for GPR activity in

  2022-07-16

  

  Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO SM-164 transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity relatio

• br Declarations of interest br Founding information

  2022-07-15

  

  Declarations of interest Founding information This work was partially supported by the New Energy and Industrial Technology Development Organization (NEDO) Japan [grant number P03043]; and Grants-in-Aid for Scientific Research [grant number 16H00738 to H.M.] from the Japan Society for the Prom

• In an effort to more fully explore

  2022-07-15

  

  In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold

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