• PBI is an agonist of

  2022-02-28

  

  PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th

• This SAR work led to the identification of compound r

  2022-02-28

  

  This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c

• LB-100 br Introduction Currently HIV infection treatment gui

  2022-02-28

  

  Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms

• Acknowledgements br Introduction Histamine mediates various

  2022-02-28

  

  Acknowledgements Introduction Histamine mediates various physiological functions and pathological actions through its interactions with histamine receptors that belong to the superfamily of seven transmembrane G-protein-coupled receptors (GPCRs) (Haas et al., 2008). Four histamine receptor subty

• Relative to the impact of moderate PAE on

  2022-02-28

  

  Relative to the impact of moderate PAE on markers of histaminergic neurotransmission, there were four salient observations from the studies reported here. First, it does not appear that moderate PAE affects the number of HDC-positive neurons in the tuberomammillary nucleus of the ventral hypothalamu

• br Acknowledgements br Introduction Type diabetes is

  2022-02-26

  

  Acknowledgements Introduction Type 2 diabetes is a progressive metabolic disorder which is characterised by chronic hyperglycaemia due to relative insulin deficiency, insulin resistance and increased hepatic glucose production [1]. The metabolism of glucose by glycolysis increases the ATP:ADP

• Spatial working memory improved in the Balb c

  2022-02-26

  

  Spatial working memory improved in the Balb/c strain at a dose of VU0410120 (i.e., 30mg/kg) that disrupted spatial working memory in the Swiss Webster comparator strain. Consistent with a recent PET study in rhesus macaques suggesting a relationship between the extent of the dose-dependent occupancy

• Although EAAT may not be involved

  2022-02-26

  

  Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few

• In the GLUT family glucose transporter

  2022-02-26

  

  In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis

• br Conclusion and future directions

  2022-02-26

  

  Conclusion and future directions GS is an important therapeutic target for the treatment of Alzheimer's disease. Its structure and function have been studied during the last years to understand the substrate cleavage mechanism to modulate the Aβ42 peptide production. The recent elucidation of GS

• br Acknowledgement This work was

  2022-02-26

  

  Acknowledgement This work was supported by National Science Foundation (21475047, 21705051, 21874048), the Science and Technology Planning Project of Guangdong Province (2016B030303010), the Program for the Top Young Innovative Talents of Guangdong Province (2016TQ03N305) and the Foundation for H

• Computational approaches such as docking and classical

  2022-02-26

  

  Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over

• br Resistance to targeted therapy The idea of treating

  2022-02-25

  

  Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target

• never br Materials and methods br Results br Discussion Dex

  2022-02-25

  

  Materials and methods Results Discussion Dex has been shown to induce apoptosis in osteoblastic cell lines (MC3T3-E1, UAMS-32 cell) [24], [25]. Consistent with previous reports, we find high-dose Dex (1 or 5 μM) can induce apoptosis of MC3T3-E1 never within 24 h as evidenced by Annexin V/P

• The inhibitory activities against HDAC and HDAC of

  2022-02-25

  

  The inhibitory activities against HDAC1 and HDAC6 of title compounds were evaluated in a fluorescent assay using SAHA and ACY-1215 as positive control. The results were displayed in A. Compounds – with linker containing 5–7 carbons showed good inhibitory activities against HDAC6. They also displayed

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