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The cytotoxicity of these compounds against Hep
2021-11-06
The cytotoxicity of these compounds against Hep3B cells was assessed using the MTT assay. As shown in , compounds in series and (except ), which retained the carboxyl at C-17, showed no appreciable cytotoxic activity (IC > 100 μM), whereas compounds in series (except ,) were modestly cytotoxic, i
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It is important to highlight that glucose dependent
2021-11-06
It is important to highlight that glucose-dependent generation of OMP of high magnitudes occurs due to the voltage-gating properties of VDACs, because only small magnitudes of OMP were obtained when the VDAC voltage sensitivity was zero (Fig. 5). These results indicate a possible physiological role
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Preadipocytes are capable of differentiating into lipid lade
2021-11-06
Preadipocytes are capable of differentiating into lipid-laden mature adipocytes. Lipid droplets are a prominent morphological feature of mature adipocytes, which is accumulated and maintained during adipocytes differentiation [26]. In this study, rHhip treatment increased lipid accumulation, as well
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The synthesis of target compound RS C
2021-11-06
The synthesis of target compound (RS)-C02 is illustrated as Scheme 2. Compound (RS)-3 was synthesized as reported procedures [40] and then reacted with ethyl piperidine-4-carboxylate to yield (RS)-C01, which subsequently was converted to target molecule (RS)-C02 by performing a nucleophilic substitu
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Aurora kinase B AURKB and haploid cell
2021-11-05
Aurora kinase B (AURKB) and haploid cell-specific protein kinase (Haspin) are two well-known participants in N-terminal histone H3 phosphorylations during mitosis. A related role played by these kinases relates to the fact that AURKB is activated by Haspin promoted phosphorylation at T3. Irrespectiv
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Recent studies on detailed biochemical and
2021-11-05
Recent studies on detailed biochemical and structural characterization of plant GSNOR Lonidamine sale confirmed their similarities to mammalian homologues [16], [17], [18], [19]. Compared to human GSNOR, plant GSNORs exhibit differences in the composition of the anion-binding pocket, which negativel
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It has been proposed that HCA may be a better
2021-11-05
It has been proposed that HCA1 may be a better target than HCA2 to treat dyslipidemia and to prevent progression of atherosclerosis, because HCA1 is less widely expressed, and HCA1 activation does not result in flushing. However, since the antilipolytic effects mediated by HCA2 appear to be not the
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br Material and methods br Results br Discussion
2021-11-05
Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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In conclusion enhanced glucagon action of the
2021-11-05
In conclusion, enhanced glucagon action of the beta cell results in improved beta cell function after glucose stimulation, but simultaneously dissociated responses to both glucose-dependent and non-glucose secretagogues evolve. This shows that the glucagon receptor is complexly involved in beta cell
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Some but not all GSIs inhibit
2021-11-05
Some, but not all, GSIs inhibit signal peptide peptidases as well, though this has not been systemically studied [36], [41]. When considering biological activities of various GSIs this is an important and understudied caveat that could influence both biological response as well as potential toxiciti
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Fpr appears to be an indispensable component of the
2021-11-05
Fpr2 appears to be an indispensable component of the signaling chain governing dendritic cell trafficking in allergic airway inflammation (Chen et al., 2010). The FPR3 agonist FL2 is chemoattractant for dendritic cells, but its biological role in vivo is yet to be defined. Within the inflammatory s
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Preliminary explorations focused on the linker of Table Lill
2021-11-05
Preliminary explorations focused on the linker of 2 (Table 1). Lilly reported that the methylene between the phenyl and the piperidyl group was metabolically susceptible to N-dealkylation, so we replaced the methylene with a carbonyl moiety to block the metabolic site [23,48] (Fig. 2). In addition,
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Through experimental models and clinical experiments those f
2021-11-05
Through experimental models and clinical experiments, those four drugs above can shown efficacy-enhancing and toxicity-reducing effects after compatibility. Our preclinical studies showed that XFC has a definite effect on relieving joint symptoms in RA patients. XFC can improve joint pain, swelling,
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The Ala to Leu substitution would
2021-11-05
The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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Dysregulation of the HPA axis resulting
2021-11-05
Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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