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In addition to the role of
2021-12-02
In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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Based on the precedent with other GlyT inhibitors
2021-12-02
Based on the precedent with other GlyT1 inhibitors such as , we evaluated both and for their ability to enhance prepulse inhibition (PPI) of the rodent acoustic startle response, a measure of sensorimotor gating known to be deficient in schizophrenic patients., In this hyPerFUsion™ high-fidelity DNA
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For the two KO models CX and CX fluorescence
2021-12-01
For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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br GSMs Secretase cleavage of
2021-12-01
GSMs γ-Secretase cleavage of APP generates a number of Aβ peptides [32], [137]. In most cells Aβ1–37, 38, 39, and 42 are produced at low levels (typically each represents 5–20% of total Aβ detected) and the major species generated is Aβ1–40 (typically over 50% of total Aβ). Other Aβ peptides can
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make film. The absence of differences between
2021-12-01
The absence of differences between GalR1 knockout and wild type mice in kainic acid-induced seizures suggests that GalR1 do not interfere with the seizure-inducing action of kainic acid. Postsynaptic kainate receptors are excitatory ionotropic glutamate receptors and their activation leads to seizu
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In addition at the spinal level results from colocalization
2021-12-01
In addition, at the spinal level, results from colocalization experiments demonstrate that GABA-C receptors are present in the substantia gelatinosa and that they are presynaptically located. Neurons located in the substantia gelatinosa are differentially activated by afferent noxious and non-noxiou
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The present data suggest that the decrease of liver
2021-12-01
The present data suggest that the decrease of liver BAs was mainly due to the decrease of hepatic BAs synthesis because the BA synthetic enzymes Cyp7a1, Cyp7b1 and Cyp8b1 were markedly reduced. The increase may also be due to the increase of hepatic BAs efflux, because the liver BA efflux transporte
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All data were analyzed using SAS software version SAS Instit
2021-12-01
All data were analyzed using SAS software (version 9.3, SAS Institute Inc., Cary, NC). Because of very low FFAR1 protein detection (at the detection limit or no signal) in 3 H-BHB cows, quantification was not possible within a linear range and therefore these animals were omitted from the statistica
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TCS JNK 5a Studies have indicated that formylated
2021-12-01
Studies have indicated that formylated peptides, FPRs, and in particular FPR-1 may be principal conductors in inflammatory processes in sterile-24, 26 and infection-related diseases. FPR-1 and formylated peptides, which are active components of CS, have been involved in smoking-induced lung damage,
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br Drug design Over the past
2021-12-01
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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In addition the interplay of membrane curvature induced tens
2021-12-01
In addition the interplay of membrane curvature induced tension at the fusion pore and TCEP induced tension across the PM seems to be a worthwhile target for investigation. The roles of dynamin and myosin II and especially their spatial and temporal dynamics during activity warrant further research
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In vitro studies have described the kinetic parameters
2021-12-01
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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As evidenced by SARs and crystallographic data HO has
2021-12-01
As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer
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The inhibition of HDAC increases the level of histone acetyl
2021-12-01
The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity a
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br Acknowledgments br Introduction Histone deacetylases HDAC
2021-12-01
Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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