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The pharmacokinetic properties of were amenable to oral
2022-06-09

The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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In this study we intended
2022-06-09

In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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Talabostat mesylate The results show that pimarane and
2022-06-09

The results show that -pimarane and -strobane diterpenoids exert inhibitory effects on FXa suggesting that they may have potential as FXa inhibitor. However, it should be noted that some compounds such as compounds , , , and are poorly bioavailable. Thus, the current study indicates that the number,
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Evidence suggests that phosphorylation increases
2022-06-09

Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin THZ1 Hydrochloride [129]. Thus, phosphor
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Previous study demonstrated that Hcy elevated
2022-06-09

Previous study demonstrated that Hcy elevated organ culture-induced up-regulation of ETB receptor in VSMCs (Chen et al., 2016a; Chen et al., 2016b). Many signaling pathways were involved in Hcy-induced up-regulation of ETB receptor in VSMCs, such as ERK1/2/NF-κB signaling pathway, Sirt1/NF-κB signal
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br Concluding Remarks One of the
2022-06-08

Concluding Remarks One of the remarkable features of Hippo signaling is its sensitivity to the cytoskeleton and mechanical forces. Progress has been made recently in identifying molecular mechanisms by which the cytoskeleton can influence Hippo signaling, but among the many outstanding questions
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Thus both in Drosophila and mammals
2022-06-08

Thus, both in Drosophila and mammals, the Hippo pathway responds to cell–cell junctions via an apical NF2/Mer-containing complex. Indeed, Hippo signalling and NF2 are required for contact inhibition of growth in cell culture, which is thought to reflect an in vivo function as a sensor of tissue crow
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Papain Previous studies have shown that HER is also
2022-06-08

Previous studies have shown that HER2 is also involved in IL-6 expression and signaling. IL-6, HER2, and GP130, the beta-subunit of the IL-6 receptor (IL-6R), are physically associated and co-immunoprecipitate in response to IL-6 stimulation [1]. IL-6 induced HER2 clustering to the GP130 complex, le
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br Methods br Involvement of HO in
2022-06-08

Methods Involvement of HO-1 in rheumatic diseases Therapeutic strategy targeted HO-1 Based on the researches focusing on the effect of HO-1 in rheumatic diseases, amount of approaches targeting regulation of HO-1 have been arising (See Table 1 for summary). It has been shown that different
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br Transparency declaration br Acknowledgements br Hepatitis
2022-06-08

Transparency declaration Acknowledgements Hepatitis C Virus (HCV) infection represents a disease of significant global impact that afflicts around 170 million people worldwide., A small proportion of infected people clear the virus naturally, whilst the majority develop chronic hepatitis C
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Toxoplasma gondii is an exceptionally tractable apicomplexan
2022-06-08

Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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Here we investigate the structural and biochemical
2022-06-08

Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or STAT5 Inhibitor a
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The role of the cyclic AMP regulated exchange factor
2022-06-08

The role of the cyclic AMP regulated exchange factor Epac1 is emerging in cancer (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). Interestingly, in cancer cell migration, activation of Epac1 can be linked to activation of Rac. As s
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br Lactate metabolism L Lactate is
2022-06-08

Lactate metabolism L-Lactate is an intermediate metabolite in glucose metabolism. Glucose can be broken down to pyruvate, and pyruvate can be either further oxidized to acetyl-CoA and enter the TCA cycle, or reduced to L-lactate by lactate dehydrogenase (LDH). In turn, LDH can oxidize L-lactate t
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procollagen c proteinase Based on these findings we set out
2022-06-08

Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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