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The molecular mechanism of gliotransmitter release
2022-03-02

The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular AZ 10606120 dihydrochloride of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores
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Recently the spectrin cytoskeleton a deformable actin associ
2022-03-02

Recently, the spectrin cytoskeleton, a deformable actin-associated network, has been identified as a modulator of Yki function, potentially acting both apically and basally in different cell types [75•, 76•, 77•]. Several mechanisms have been proposed, including regulation via Crb/Ex tethering [], t
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Activation of sGC induces the generation of cyclic guanosine
2022-03-01

Activation of sGC induces the generation of cyclic guanosine monophosphate (cGMP), phosphorylation of protein kinase G (PKG) and changes in activity of effector proteins such as phosphodiesterases (PDE), ion channels and ion pumps [43]. This pathway eventually leads to dilation of GSK2118436 mg (br
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br All platelet agonists acting through specific
2022-03-01

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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An interesting question is why RhoF
2022-03-01

An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino valeriana te receptor mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF
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Based on the role of NMDA
2022-03-01

Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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In three groups independently proposed two different mechani
2022-03-01

In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit
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We recently reported the first cyclopropene analog of the am
2022-02-28

We recently reported the first cyclopropene-analog of the amino green neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [28]. We obt
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AKR D is very highly expressed in
2022-02-28

AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv
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The in vivo biological activity
2022-02-28

The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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Analogous to all GPCRs the GLP R transduces signals from
2022-02-28

Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva
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It was recently reported that aged
2022-02-28

It was recently reported that aged GHSR−/− mice, in addition to showing alterations in meal pattern microstructure, exhibit NPY and AgRP mRNA upregulation in the ARC [56]. After an overnight fast, our animals exhibited a similar pattern of upregulated NPY and AgRP mRNA expression. Given that GHSR1a
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The role of GJs in
2022-02-28

The role of GJs in liver fibrogenesis was studied recently. Studies showed a significant decrease in liver fibrosis in Cx32 knockout mice compared to wild-type mice. Although the mechanism underlying this protective effect of Cx32 deletion is not clear, reduced oxidative stress was suggested as a po
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PK profiles of were evaluated and found
2022-02-28

PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 c
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br Site of expression FASTK is expressed in various parts
2022-02-28

Site of expression FASTK is expressed in various parts of human body including heart, skeletal muscle, brain, placenta, lung, liver, kidney pancreas (Ota et al., 2004) and many other organs (Fig. 1). It has been reported that FASTK is highly expressed in pancreatic tumors, where it is involved in
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