• It is important to note that histamine H and

  2022-05-19

  

  It is important to note that histamine H1 and H2 receptors are coupled to different G proteins and that their crossinterference induced by histamine H1 and H2 receptor inverse agonists depends on the cointernalization mechanism. To date, histamine H1 and H2 receptor inverse agonist have shown to int

• Furthermore we observed a striking difference between

  2022-05-18

  

  Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic ckit type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of sGC. In combinatio

• Introduction Glycogen synthase kinase GSK is an enzyme playi

  2022-05-18

  

  Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and Exemestane synthesis is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsolida

• A similar symbiotic relationship has

  2022-05-18

  

  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

• In summary we have designed and

  2022-05-18

  

  In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr

• The original Bee Synch methodology now termed Bee Synch

  2022-05-18

  

  The original Bee Synch methodology (now termed Bee Synch I) utilizes a 5-day CIDR, GnRH (GnRH-1) and PGF on day 0, double dose of PGF on day 5, and FTAI with GnRH (GnRH-2) at 66 h after CIDR removal. Cruppe et al. (2014) reported that the inclusion of GnRH on day does not contribute appreciably to f

• Rapid action of E on GnRH neurons

  2022-05-18

  

  Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor

• During the structural transition the FD the PHD and the

  2022-05-18

  

  During the structural transition, the FD, the PHD and the TrD retain their tertiary structure. Nevertheless, they undergo large rearrangements in their relative orientation due to secondary changes in hinge segments (R1 to R5) which refold during the low-pH induced conformational change. Particularl

• In response to oxidative stress in DM antioxidant defence

  2022-05-18

  

  In response to oxidative stress in DM, antioxidant defence systems are activated in β-cells. Glutathione (GSH) is one of the most abundant antioxidants and has been shown to be expressed at lower concentrations in patients with DM [12], [13]. Furthermore, plasma levels of glycine, which is a synthet

• br Vesicular glutamate transporters VGLUTs br Conclusions Du

  2022-05-18

  

  Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,

• Introduction Glucose is the most important energy carrier of

  2022-05-18

  

  Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula

• Genetic disruption or pharmacologic inhibition of the

  2022-05-18

  

  Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co

• br In vivo actions of GLP GLP R agonists

  2022-05-18

  

  In vivo actions of GLP-1/GLP-1R agonists on the vascular endothelium Using contrast-enhanced ultrasound, male Sprague Dawley rats receiving an intravenous infusion of native GLP-1 (30 pmol/kg/min) for 2 h demonstrated significant improvements in both microvascular blood volume and microvascular b

• The presented results speak for the direct effects of ghreli

  2022-05-18

  

  The presented results speak for the direct effects of ghrelin on rat spermatozoa, which are accomplished by the activation of the GHSR-1a receptor. Thus, the results seem to be of physiological significance in vivo since ghrelin, the natural ligand of GHSR-1a, was found to be present in the seminal

• We reviewed the results of comprehensive genomic profiling

  2022-05-17

  

  We reviewed the results of comprehensive genomic profiling (CGP) in 26,054 cases of NSCLC and examined the frequency and clinical characteristics of patients whose tumors harbor FGFR fusions. To our knowledge, this is the most in-depth evaluation of FGFR fusions exclusively in NSCLC. Here we will de

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