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Introduction Cancer has been a significant public health pro
2021-10-16
Introduction Cancer has been a significant public health problem in the world with more patients being diagnosed every year. However, chemotherapy from non-specific cytotoxic agents that as an effective means of cancer treatment is limited by severe side effects and poor selectivity. Thus, the deve
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Paxilline IC is a rat mAb specifically
2021-10-16
IC2 is a rat mAb specifically binding to insulin granula [127,128]. Although this mAb was discovered 30 years ago, it has only recently been used for β-cell imaging in vivo. Moore et al. used this mAb for β-cell imaging in 2001 [129]. After DTPA conjugation, IC2 was labeled with 111In. Both in vitro
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TGR is a class A
2021-10-16
TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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br Expression of GlyT in the
2021-10-16
Expression of GlyT in the spinal cord in response to neuropathic pain Twelve days after sham injury or CCI, GlyT1 and GlyT2 mRNA expression in rat spinal cord was analyzed using qPCR. Here, no significant changes in expression of the transporters in our CCI model of neuropathic pain compared wit
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br Materials and methods br
2021-10-16
Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast LY 2389575 hydrochloride mg by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs
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Human Glucocorticoid Receptor hGR was first cloned in
2021-10-16
Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin
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Rofecoxib The second experiment investigated the
2021-10-15
The second experiment investigated the possible neuronal mechanism underlying the effect of acupuncture. The baseline level of methamphetamine consumption in each group was similar, as in the first experiment (Fig. 2A). Acupuncture at HT7 also significantly inhibited the methamphetamine self-adminis
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In single channel studies Zn
2021-10-15
In single channel studies, Zn2+ primarily inhibits GABA-A receptors through the reduction of channel opening probability (Smart, 1992, Smart et al., 1994). In slice recordings, Zn2+ significantly reduces phasic mIPSC event amplitude and kinetics, as well as desensitization kinetics (Barberis et al.,
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FXa is a vitamin K dependent serine protease
2021-10-15
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Cy5 EGFP mRNA and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The a
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Type IIIa b the ligand dependent oncogenic
2021-10-15
Type IIIa/b – the ligand dependent oncogenic Hh pathway (paracrine or reverse paracrine mode) is mediated by paracrine activation and is usually encountered in embryonic development, but also in installation and progression of cancer [58]. Specifically, Hh ligands secreted by malignant Aclacinomycin
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Screening of the compounds allowed for a
2021-10-15
Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detr
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In the present study we showed
2021-10-15
In the present study, we showed that reduced neuron formation in vitro induced by IL-1β was ameliorated by activation of GPR55 in both human and mouse cultures of NSCs. Pre-treatment with GPR55 agonists also blocked upregulation of inflammatory cytokine receptor mRNA (IL-1R1, IL-6st) while increasin
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Heparin and suramin are highly negatively
2021-10-15
Heparin and suramin are highly negatively charged molecules, and they are in this aspect, similar to DNA and likely to compete with DNA by binding to the protein cationic groups [17] (Fig. 1). The inhibitory effect of heparin and suramin on DNA and RNA binding proteins has been described [[18], [19]
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br Materials and methods br Results
2021-10-15
Materials and methods Results Discussion Here, we investigated the inhibitory effects and associated mechanisms of phloroglucinol on α-glucosidase. Our results showed that phloroglucinol reversibly inhibited α-glucosidase in a dose-dependent manner (Fig. 1), with the double-reciprocal plot
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br Vertebrate steroid receptor evolution br Conclusion The
2021-10-15
Vertebrate steroid receptor evolution Conclusion The teleost WGD event resulted in the duplication of the vertebrate GR and MR and two GRs have been retained in the majority of teleost fish studied so far. The molecular basis for this retention has yet to be fully understood. The cloning of th
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