• A similar symbiotic relationship has

  2022-02-22

  

  A similar symbiotic relationship has been reported in the brain, where increased gradients of lactate secreted by astrocytes enables neurons to import and use this nutrient, a process referred to the ‘neuron–astrocyte lactate shuttle’ [16]. Similarly, lactate-based metabolic coupling established by

• The Bcl and Bcl xL genes contain the CRE binding

  2022-02-22

  

  The Bcl-2 and Bcl-xL genes contain the CRE binding site in their promoter regions for CREB and CBP to bind to, so CREB phosphorylation was shown to up-regulate these anti-apoptotic genes, Bcl-2 and Bcl-xL [[29], [30], [31]]. Bcl-2 and Bcl-xL prevent the activation of caspases and the release of mito

• The pharmacokinetics of was obtained

  2022-02-22

  

  The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indicat

• To shed more light on the

  2022-02-22

  

  To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ

• The CO chemosensitivity of the LH

  2022-02-22

  

  The CO2 chemosensitivity of the LH/PFA has been shown to be dependent on sleep-wake states (B.S. Deng et al., 2007; Dias et al., 2010, 2009; Li et al., 2013). In this context, it was demonstrated that focal acidification of the LH/PFA, by microdialysis of acidic artificial cerebrospinal fluid (aCSF)

• Through the analysis of various synthetic GPR agonists

  2022-02-22

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic BQ-788 sodium salt motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of disco

• At the second step blind docking

  2022-02-22

  

  At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se

• br Experimental br Results br Discussion The

  2022-02-22

  

  Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,

• br Acknowledgements br Introduction High intensity

  2022-02-22

  

  Acknowledgements Introduction High-intensity noise exposure has long been known to induce damage in the peripheral and central auditory system, often resulting in auditory pathologies such as hearing loss, tinnitus and hyperacusis (Syka, 2002; Roberts et al., 2010). Within the inner ear, struc

• br Methods br Results Top panels

  2022-02-22

  

  Methods Results Top panels of the Fig. 1 show the conventional representation of the predicted values of TL,CO according to ERS’93 and GLI′17 as a function of age and keeping the height constant (160 cm, panel A and 190 cm, panel B). This figure shows that the GLI-‘17 predicted values of TL,CO

• More polar substituents introduced on the

  2022-02-22

  

  More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m

• br Introduction Farnesoid X receptor

  2022-02-21

  

  Introduction Farnesoid X receptor (FXR) is a bile apigenin sale regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that

• br Material and methods br Acknowledgements and

  2022-02-21

  

  Material and methods Acknowledgements and funding The authors thank Katharina Elsässer for technical support and Emma Esser for careful editing of the manuscript. We also thank Marcus Conrad for providing Liproxstatin-1 and advisory comments and discussion on the manuscript. This work was part

• br Rationale The present study was motivated to get further

  2022-02-21

  

  Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym

• In vitro studies have described the kinetic

  2022-02-21

  

  In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value

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