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A second feature of the Ras type
2022-02-08

A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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One important aspect about GSK inhibitors
2022-02-08

One important aspect about GSK-3 inhibitors is their effect on pluripotency of AG-490 [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of events preserve
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br Author contributions Animal experiments real time PCR and
2022-02-08

Author contributions Animal experiments, real time PCR and western blots were performed at the Department of Physiology, CIMUS, University of Santiago de Compostela and Department of Cell Biology, Physiology and Immunology, Instituto Maimónides de Investigaciones Biomédicas (IMIBIC) / Reina Sofia
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Using RT PCR we demonstrated the expression of
2022-02-08

Using RT-PCR we demonstrated the expression of GPR55 receptor mRNA in the ileum and colon of mice, which is in good agreement with previous reports (Lin et al., 2011). The quantitative analysis showed the abundance of GPR55 mRNA in the mucosa of the ileum and colon. In contrast, in LMMP preparations
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Thalidomide Several studies have found that GPR possesses a
2022-02-08

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Thalidomide expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (
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Restless running behavior was first described in mice after
2022-02-07

‘Restless running behavior’ was first described in mice after administration of 30mg/kg i.p. ALX-5407 and was thought to be due to an augmentation of NMDA-induced dopamine activity [27]. The motor impairments caused by ALX-5407 were confirmed by Perry et al. [10] and extended to another sarcosine-de
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A number of experimental data declare a tight
2022-02-07

A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in Bay 65-1942 HCl salt receptor and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Be
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In this study we investigated the contribution
2022-02-07

In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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In the present study we set
2022-02-07

In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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p2x receptors In the course of our synthetic studies we
2022-02-07

In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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br Acknowledgments The authors gratefully acknowledge the
2022-02-07

Acknowledgments The authors gratefully acknowledge the support provide by National Natural Science Foundation of China (Number 31301415). Introduction β-Galactosidases (EC 3.2.1.23), frequently known as lactases, are widely used in lactose hydrolysis. This disaccharide is present in mammalian
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Galactosidase Gal EC is an enzyme exoglycosidase and
2022-02-07

α-Galactosidase (α-Gal, EC 3.2.1.22) is an enzyme exoglycosidase, and the main role of this enzyme is the enzymolysis of α-galactoside. After this hydrolysis, galactosylation of cyclodextrins by the α-galactosidase occurs, thus forming α-galactosyl-cyclodextrin. This branched CD is easy to dissolve
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The PK and the tissue
2022-02-07

The PK and the tissue distribution profiles of 15k, 15j, 14d and 2 (Table 8) in male ICR mice were assessed. 15k, 15j, 14d all exhibited prolonged half-lives and improved plasma exposure. 15k achieved the highest concentration (15.45 μg/mL) in plasma among four compounds. The observation that 15j (S
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To further investigate if GPR was the functional target
2022-02-07

To further investigate if GPR40 was the functional target of these phenylpropiolic GW9662 analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40 ce
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br Introduction Atrial fibrillation is the most common cardi
2022-02-05

Introduction Atrial fibrillation is the most common cardiac arrhythmia (Benjamin et al., 1998). Pulmonary vein (PV) sleeves contain a mixture of working myocardium and potential arrhythmogenic pacemaker CGP 42112 receptor behaving as an ectopic trigger of atrial fibrillation (Haissaguerre et al.
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