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A number of anti diabetic drugs are available
2022-02-14
A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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WAY-600 br Introduction Maintaining blood glucose within an
2022-02-14
Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The WAY-600 is especially dependent on an adequate, continuous supply of circulating glucose to fuel
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Previous researches about ghrelin focused primarily
2022-02-14
Previous researches about ghrelin focused primarily on gastrointestinal functions [30], energy balance [31], weight [32], and more recently on anxiety [33], [34], [35] and depression [36]. Here, we provided the first demonstration that chronic peripheral or central ghrelin treatment to CUMS rodents
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More polar substituents introduced on the
2022-02-14
More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in mic
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Two typical properties of Gi o protein coupled receptors nam
2022-02-12
Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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br Acknowledgment S A was
2022-02-12
Acknowledgment S.A was supported by V Plan Propio US-Acceso USE-14793-G. Introduction The Hippo signaling pathway is an evolutionarily conserved pathway that controls organ size and cell differentiation across diverse organisms through the regulation of cell proliferation and apoptosis (Di Ca
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In vitro studies suggest that the increase in Hx
2022-02-12
In vitro studies suggest that the increase in Hx activity seen in normal pregnancy may contribute to the down-regulation of the vascular expression of Angiotensin II receptor 1 thereby promoting a relaxed and dilated maternal vascular bed [25]. It has further been suggested that the decreased Hx act
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After establishing improved GSNOR potency some of
2022-02-12
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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br Conflict of interest statement br Acknowledgments The aut
2022-02-12
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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Compared to methadone or morphine buprenorphine is a partial
2022-02-12
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of dev
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The calculations for the R
2022-02-12
The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn A-54556A is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchanged roles o
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It is becoming increasingly apparent that membrane
2022-02-12
It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene
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Our study has some limitations that should be considered whe
2022-02-12
Our study has some limitations that should be considered when the results are interpreted. First, we did not measure the protein levels of Bax and Bcl2, due to time and budget limitations. Although simultaneous measurements of both mRNA and protein levels are complementary for a better understanding
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uPAR another newly discovered ligand has implicated FPRL as
2022-02-12
uPAR, another newly discovered ligand, has implicated FPRL1 as a potential link between the fibrinolytic cascade and inflammation. uPA is a serine protease best known for its ability to regulate fibrinolysis and for its importance in tissue remodeling and tumor invasion [49]. However, uPA also induc
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It is noted that knee swelling was milder and
2022-02-12
It is noted that knee swelling was milder and the intensity of IL-4 staining (MFI) in the vehicle-treated group was lower in the second (Fig. 7a and d) than the first (Figs. 1a and 3f) AIA experiment. The variation in joint swelling between the two studies is most likely due to the models being perf
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