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Chidamide An increased sympathetic tone and the hormone gluc
2022-02-18

An increased sympathetic tone and the hormone glucagon are the main glucose mobilizing factors [28], [29]. Single-cell transcriptome analysis of human islet cells suggests the expression of Ffar1 not only in β-cells but also in α-cells [30]. Moreover, analysis of rat α-cells indicates that FFAR1 exp
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The third generation cephalosporin antibiotics can cross the
2022-02-18

The third-generation cephalosporin what does cytoskeleton do can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when tak
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AKR D is very highly expressed in human
2022-02-18

AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv
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FXR agonists represent an attractive class of drugs for pati
2022-02-18

FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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The fibroblast growth factor receptor FGFRs
2022-02-18

The fibroblast growth factor receptor (FGFRs), including four highly conserved proteins (FGFR1-4), are important membrane sensors for extracellular signals [4]. By binding to their ligands, FGFRs are activated and can trigger various downstream intracellular signaling cascades, which is required for
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br Material and methods br Results br Discussion In
2022-02-18

Material and methods Results Discussion In the present study, we attempted to unravel the mechanism underlying the statin-mediated inhibition of FGFR3 signaling in chondrocytes, reported earlier by Yamashita and colleagues. We evaluated the role of statins in four different experimental sys
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Glucose induced nuclear translocation of several enzymes inc
2022-02-18

Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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br Materials and methods Unless stated
2022-02-18

Materials and methods Unless stated otherwise, all chemicals were from Sigma-Aldrich and were of the cell culture grade. HL-1 cardiomyocytes were presented by Dr. W.C. Claycomb (Louisiana State University Health Science Center, New Orleans, LA, USA) [8]. Results and discussion Acknowledgeme
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Over of all melanomas have activating
2022-02-18

Over 50% of all melanomas have activating BRAF mutations [29] and inhibition of the Ras/Raf/MEK/ERK signaling pathways is one of the most promising treatments for malignant melanoma [30]. However, studies using BRAF inhibitors have identified various feedback mechanisms to activate BRAF pathway in m
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br Materials and methods br Results and discussion br Conclu
2022-02-18

Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka
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In addition to indoles two
2022-02-18

In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic LY 2389575 hydrochloride side chain to prepare compound (). The extension of
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Structurally HMTs can be broadly categorized
2022-02-18

Structurally, HMTs can be broadly categorized into three functional enzymatic families, the SET (Suppressor of variegation, Enhancer of zeste, Trithorax)-domain- containing methyltransferases, the non-SET DOT1-like (DOT1L) lysine methyltransferases, the PRDM family, containing a PR (PRDI-BF1-RIZ1 ho
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br Acknowledgments br Introduction The incidence
2022-02-17

Acknowledgments Introduction The incidence of cholangiocarcinoma (CCA), a malignant tumor found in both intra- and extra-hepatic biliary epithelia [1], has been increased worldwide over the past two decades [2]. The prognosis of CCA patients are generally poor, due to the lack of early detecti
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br Materials and methods br Results br Discussion and conclu
2022-02-17

Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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The two competitive bivalent GlxI inhibitors
2022-02-17

The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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