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br The mode of binding of ligands to GPR As
2021-09-17
The mode of binding of ligands to GPR35 As noted above, although kynurenic Miltefosine is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importantly, in
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Glycine regulates several brain functions
2021-09-17
Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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On the other hand we have previously demonstrated that gelse
2021-09-17
On the other hand, we have previously demonstrated that gelsemine displaced the H3-strychnine from membrane fractions of rat spinal cord homogenates. In addition, spinal gelsemine antinociception was blocked by intrathecal injection of the specific glycine receptor antagonist strychnine or gene sile
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FFAR is highly expressed not
2021-09-17
FFAR1 is highly expressed not only in β cells but also in α ccgs (Segerstolpe et al., 2016), which gives the interesting perspective that 20-HETE may function both as an autocrine and as a paracrine regulator of islet cell function (Figure 1A), i.e., acting in symphony with the many other intra-isl
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To further implicate the role of EAAT in morphine
2021-09-17
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 triptolide was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice a
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br Introduction The glucagon receptor GCGR is a G
2021-09-17
Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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Emergent studies have recently shown that
2021-09-17
Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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The Cx family of integral
2021-09-17
The Cx family of integral membrane proteins [13] are key components of the Gap Junction channels that provide GJIC, which is indispensable in the preservation of tissue integrity and homeostasis in multicellular organisms. Gap Junction channels form a conduit for exchange of ions (Ca2+), second mess
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Galanin mediates its activity by binding to
2021-09-17
Galanin mediates its activity by binding to three G-protein coupled receptor subtypes (designated GAL1-GAL3). Since GAL3 mRNA is found mainly in regions of the mesolimbic dopamine system, such as the ventral tegmental area, dorsal raphe nucleus, LC, amygdala, hippocampus, thalamus, hypothalamus, NAc
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Interestingly we have shown that OA required FFAR to
2021-09-17
Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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br FGF FGFR pathway as predictive factor
2021-09-17
FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9 m
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Compounds were tested for GPR
2021-09-17
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO ER 27319 maleate sale 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 structur
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Liver and muscle isozymes have been found in
2021-09-17
Liver and muscle isozymes have been found in vertebrate tissues [2], [5], [6]. The liver FBPase is recognized as a regulatory enzyme of gluconeogenesis. The muscle isozyme participates in the glycogen synthesis from lactate and in the regulation of glycolysis [7], [8], [9]. The basic difference betw
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A pyrimidine class of compounds is of enormous interest with
2021-09-17
A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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br Introduction Hexokinase HK is an enzyme
2021-09-16
Introduction Hexokinase (HK) is an enzyme that catalyses the transfer of phosphate from ATP to glucose in the first step of glucose metabolism (Wilson, 1995, Wilson, 2003). In mammalian, HK has four important isozymes which are designated as HK1, HK2, HK3 and HK4 (Wilson, 1995, Wilson, 2003). HK1
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