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GSK is inhibited by serine phosphorylation at a
2022-02-09
GSK-3 is inhibited by serine trabectedin at a residue its N-terminus (Ser 9 in GSK-3β and Ser 21 in GSK-3α) [52], [53], [54]. This raised the possibility that the N-terminal tail may function as a pseudo-substrate by mimicking the pre-phosphorylated substrate. The interaction mode of the pseudo-subs
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The endocannabinoid system ECS consists of cannabinoid CB
2022-02-09
The endocannabinoid system (ECS) consists of cannabinoid (CB)1 and CB2 receptors, their endogenous ligands anandamide and 2-arachidonylglycerol, and the synthesizing and degrading enzymes for these ligands. Cannabinoids and the ECS are involved in the regulation of GI motility in physiological and p
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There is no doubt that GPR is a
2022-02-09
There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago
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br Acknowledgments br Introduction Myelin one of the fundame
2022-02-09
Acknowledgments Introduction Myelin, one of the fundamental adaptations of vertebrates, is a multilamellar structure deriving from the spiral wrapping around the Ranolazine of the plasma membrane of myelin forming glia, oligodendrocytes in the central nervous system and Schwann cells (SC) in
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ATP as a transmitter can be released from injured
2022-02-09
ATP as a transmitter can be released from injured fda approved and sensory nerve endings (Sperlágh et al., 1995, Sperlágh et al., 1997, Sperlágh et al., 1998, Burnstock, 2013, Burnstock, 2014). ATP can activate the P2X3 receptor in the DRG neurons (Gao et al., 2011a; Xu et al., 2012). In DRG neuron
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br Characterization and regional localization of Glu transpo
2022-02-08
Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr
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Further insight in how exactly galanin
2022-02-08
Further insight in how exactly galanin might inhibit seizures was obtained from galanin transgenic mice. It occurred that the altered susceptibility to seizures was in direct correlation with glutamate release from hippocampal slices obtained from these animals (Fig. 2(b)). While no differences were
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Introduction galactosidase d galactoside galactohydrolase or
2022-02-08
Introduction β-galactosidase (β-d-galactoside galactohydrolase or lactase; EC 3.2.1.23) is an important type of glycoside hydrolase that can catalyze the conversion of lactose to TNF-alpha, recombinant human protein and galactose. Furthermore, it can also catalyze transglycosylation reactions, whi
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br G protein coupled receptor GPR also known
2022-02-08
G-protein coupled receptor 40 (GPR40), also known as a free fatty calculate concentration receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GP
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BH3I-1 sale br Introduction A great many isoprenoids with va
2022-02-08
Introduction A great many isoprenoids with varieties of structural diversity, such as steroids, carotenoids, prenyl quinones, and natural rubber, occur in nature. All of these biosynthetic precursors are constructed by the action of prenyl chain elongating enzymes [1], [2], [3], [4]. These enzyme
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Histamine H and H receptors are considered
2022-02-08
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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In the adult normal spinal cord the resident cells
2022-02-08
In the adult normal spinal cord, the resident cells mainly include neurons, astrocytes, oligodendroglia and microglia (Lecca et al., 2012, Miyagi et al., 2012). After SCI, the lesion microenvironment is complex, which includes the functional changes of CNS resident cells and the infiltration of leuk
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While the specific set of challenges
2022-02-08
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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In the present study we found that the expression
2022-02-08
In the present study, we found that the expression of GPR120 in decidua from women of spontaneous abortion was significantly downregulated compared to the decidua from that of normal pregnancy. Moreover, GPR120 deletion (GPR120−/−) or inhibition predisposed mice to LPS or RU486 induced abortion, ind
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Taxifolin br Introduction Over the past two decades the prev
2022-02-07
Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life
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