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br Conclusion br Introduction The intracellularly generated
2022-04-16

Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri
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The observed increase in macroscopic conductance
2022-04-15

The observed increase in macroscopic conductance could be due to a left shift in the open state probability vs. voltage curve for the high-activity state causing an increase in the open state probability at all potentials. However, an increase of the apparent single channel conductance cannot be ent
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HCC metastasis is a multistep multifactorial process
2022-04-15

HCC metastasis is a multistep, multifactorial process, including adhesion of tumor Gedunin to the extracellular matrix (ECM), remodeling and degradation of ECM, invasion through local tissue, intravasation into blood or lymph vessels, and forming new tumors at distant sites [6,7]. Loss of adhesion
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The primary cancer lesion was mostly in the
2022-04-15

The primary cancer lesion was mostly in the uterus and adnexa, followed by the gastrointestinal tract, brain, blood, and kidney and Thalidomide (Fig. 2A). Histopathological findings indicated that most cancers were adenocarcinomas, followed by squamous cell carcinomas, glioblastomas, malignant lymp
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The present experimental study identified remarkable protect
2022-04-15

The present experimental study identified remarkable protective effects for celecoxib against renal toxicity caused by CSA. All aspects of CSA nephrotoxicity, functional, inflammatory, fibrotic, and structural, were improved by celecoxib. Mechanistically, pharmacological and immunostaining protein e
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Two typical properties of Gi o
2022-04-15

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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Arena Pharmaceutical introduced a biaryl sulfone derivative
2022-04-15

Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Intestinal epithelium renewal is tightly controlled by Hedge
2022-04-15

Intestinal epithelium renewal is tightly controlled by Hedgehog genes. Three Hedgehog genes are highly conserved in mouse and human, including Sonic hedgehog (Shh), Indian hedgehog (Ihh), and Desert hedgehog (Dhh) [13]. Hedgehogs bind to Patched (PTCH) [[14], [15], [16]], which unlike conventional r
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6656 Based on pharmacophore modeling a good
2022-04-15

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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Ning et al showed that LPC appeared to increase insulin
2022-04-14

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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In prostate cancer PCa glucose metabolism plays a major
2022-04-14

In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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This study was approved by
2022-04-14

This study was approved by our institutional ethics committee, and informed consent was obtained from each participant or legal guardian. We performed whole-genome SNP genotyping in the one unaffected and two affected siblings by using the Illumina Human 610 Genotyping BeadChip panel, which interrog
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8-pCPT-2-O-Me-cAMP-AM The eradication of agonist activity in
2022-04-14

The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary 8-pCPT-2-O-Me-cAMP-AM as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also
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The OTR and GHSR are known to play similar roles
2022-04-14

The OTR and GHSR are known to play similar roles in centrally regulated behaviours, where the OTR is implicated in mood, sociability and appetite regulation (Morton et al., 2012; Myers et al., 2014; Sala et al., 2013; Lukas et al., 2011; Slattery and Neumann, 2010), with the GHSR primarily involved
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Based on the above considerations the galactosidase gene fro
2022-04-13

Based on the above considerations, the β-galactosidase gene from Exiguobacterium acetylicum MF03 (not previously reported) was cloned, expressed and purified with the aim of assessing the potential of this novel enzyme for catalyzing reactions of synthesis and hydrolysis of glycosides. Because of E.
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