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SGLT inhibitors have been accepted as
2022-07-21
SGLT-2 inhibitors have been accepted as a new class of antidiabetic agent (Kurosaki and Ogasawara, 2013). They limit renal glucose reabsorption and promote urinary excretion of glucose, thereby reducing plasma glucose levels (de Leeuw and de Boer, 2016, Jojima et al., 2016, Pérez López et al., 2010,
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Herein in consider of the high similarity
2022-07-21
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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GHSR A s have high levels of
2022-07-21
GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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To improve the preferential GalR binding we synthesized
2022-07-21
To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollen
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When we compared the effects in FST
2022-07-21
When we compared the effects in FST induced by GAL and GAL(1–15), we observed that the increase in the immobility induced by GAL(1–15) was significantly higher than the one induced by GAL (Millon et al., 2015). Moreover, in climbing behaviour, GAL(1–15) also induced a stronger decrease in climbing r
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To ensure the induction of CYP
2022-07-21
To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme
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Knock out mice of FXR showed
2022-07-21
Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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The present data suggest that the decrease of liver
2022-07-21
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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In the phylum Cnidaria which separated from the
2022-07-21
In the phylum Cnidaria, which separated from the main line of Metazoa early during evolution, FGFR signaling is essential during development and morphogenesis. Two FGFRs and two FGFs antagonistically control formation of the apical organ in the anthozoan Nematostella and target the MAPK pathway (Ren
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br Declaration of interest br Acknowledgments br This
2022-07-21
Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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Immunohistochemistry using anti FFAR antibodies revealed imm
2022-07-21
Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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Furthermore rs is the one
2022-07-21
Furthermore, rs17171119 is the one which is studied well so far. One of the earlier studies has reported the clinical outcome and impact of EZH2 SNPs (rs41277434, rs3757441, rs2302427 rs9177211 T> C) (Crea et al., 2012). The only coding SNP ID rs2302427 has been studied in various diseases such as h
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As an inflammatory mediator histamine plays a pivotal role i
2022-07-20
As an inflammatory mediator, histamine plays a pivotal role in nociceptive processes in both the central and peripheral nervous systems (Gemkow et al., 2009; Hough & Rice, 2011; Tiligada et al., 2009). In this respect, the participation of H3Rs in modulating pain, especially neuropathic pain, has at
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Cell cell junction proteins were the
2022-07-20
Cell-cell junction proteins were the first upstream modules to be characterized as contact sensors through the Hippo pathway. These junctions may be divided in 2 categories: adherens and epithelial polarity junctions. The establishment of intercellular contacts involves the cadherin proteins present
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Aberrant expression of HKII may be a required feature
2022-07-20
Aberrant expression of HKII may be a required feature for cancer development and progression. Overexpression of HKII has been reported in tumor tissues of cancer patients with liver [9], ovary [8], [24] and larynx [25]. The clinical significance of HKII in cancer was noted as overexpression of HKII
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