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Increasing evidence has shown that
2021-12-13

Increasing evidence has shown that blockade of glutamate uptake leads to aberrant behavioral consequences. For example, intracerebroventricular (i.c.v) injection or microinjection of the GLT-1 inhibitor, dihydrokainic MHC class II antigen (45-57) [Homo sapiens] australia (DHK), into the prefrontal
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Shikonin represents naphtoquinonic compound isolated from th
2021-12-13

Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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GKRP binds to the inactive super open conformation
2021-12-13

GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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The regulation of gap junction connexin mediated activities
2021-12-13

The regulation of gap junction-connexin-mediated activities may be achieved through action on the channel gating properties (membrane voltage, pH, interaction with junctional and cytoskeletal proteins, Ca2+ and K+ concentrations, etc) or on the trafficking, turnover and localization of connexins. Sh
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Cyclopamine a steroidal alkaloid type secondary metabolite f
2021-12-10

Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas
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Next we asked how a common activation
2021-12-10

Next, we asked how a common activation marker of fibroblasts, Acta2, defined gene expression signatures in alveolar airspaces by using Acta2-mKO1 reporter mice (Fig. 2A). In the lungs of Acta2-mKO1 mice, mKO1 was expressed in smooth muscle cells and mesenchymal cells in puromycin selection concentra
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Ghrelin receptors in non mammals are reportedly
2021-12-10

Ghrelin receptors in non-mammals are reportedly more “complicated/complex and diverse” than in mammals, having additional paralogs and splice variants (Kaiya et al., 2014). Several teleost fish GHS-Rs have been identified; however, functional characterization has been conducted in only a few (see, K
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Prion diseases are transmissible and
2021-12-10

Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in angiogenesis lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can fo
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As illustrated in among all
2021-12-10

As illustrated in , among all synthesized compounds, biphenyl derivatives , , , , and with substitutions at the 3-position possessed the best FAAH inhibitory capacity. These 5 compounds demonstrated a good activity against FAAH with IC values in a submicromolar range. Nevertheless, when replacing t
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nf-κb inhibitor In conclusion the present study shows that t
2021-12-10

In conclusion, the present study shows that the endothelin system is of importance in the cardiopulmonary vascular pathophysiology of porcine endotoxin shock. In this model, combination of a selective endothelin ETA and a selective endothelin ETB receptor antagonist markedly improved pulmonary circu
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With the aim to identify potential novel
2021-12-10

With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum
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Work is presently underway to unveil mechanisms whereby SAHA
2021-12-10

Work is presently underway to unveil mechanisms whereby SAHA-dependent restoration of cardiomyocyte autophagic flux is protective. Another interesting question pertains to mechanisms whereby class I and class II HDAC inhibitors induce autophagy. It has been demonstrated that TSA reduces transverse
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b-raf inhibitors Here we used chemogenetic modulation of
2021-12-09

Here, we used chemogenetic modulation of MBH GHSR neurons to address the role of the endogenous ghrelin system in the normal, hyperphagic response to a short-term fast. Studies demonstrating the requirement of an intact ghrelin-GHSR system for the rebound food intake following fasting have been inco
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ETV plays an important role in tumorigenesis and
2021-12-09

ETV5 plays an important role in tumorigenesis and metastasis. For example, chromosomal rearrangement of ETV5 which results in increased ETV5 level is believed as a common event driving human prostate cancer (Helgeson et al., 2008; Huang and Waknitz, 2009). Ghrelin/acyl-ghrelin also plays an importan
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The Cx family of integral
2021-12-09

The Cx family of integral membrane proteins [13] are key components of the Gap Junction channels that provide GJIC, which is indispensable in the preservation of tissue integrity and homeostasis in multicellular organisms. Gap Junction channels form a conduit for exchange of ions (Ca2+), second mess
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