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GPR A a G protein coupled receptor
2021-10-19
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic MK2 inhibitor [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-medi
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Four polymorphic variants of Neil namely S
2021-10-19
Four polymorphic variants of Neil1, namely, S82C (rs5745905), G83D (rs5745906), C136R (rs5745907) and D252N (rs5745926) were characterized by Roy et al. in 2007 (Table 1). Analyses of AP site incision on Tg containing oligonucleotide showed that S82C and D252N variants had wild type activity and car
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A major hurdle in purifying a
2021-10-19
A major hurdle in purifying a membrane protein is finding a detergent that can preserve the protein, after releasing it from a given membrane, in a stable and non-aggregated state during purification steps [18,50]. The ability of various detergents used to solubilize and purify membrane proteins has
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Ning et al showed that LPC appeared
2021-10-19
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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High lipophilicity of seems to cause poor
2021-10-18
High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i
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Here we report a new human
2021-10-18
Here, we report a new human genetic disorder in a patient with hypoalgesia, altered fear and memory symptoms, and a non-anxious disposition. This disorder is attributable to co-inheritance of a microdeletion in a novel pseudogene and a known FAAH hypomorphic SNP. The microdeletion is flanked by repe
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PKC does not however directly stimulate secretion
2021-10-18
PKC does not, however, directly stimulate secretion by initiating calcium influx into the cell [51]. Work from multiple groups measuring calcium currents has shown that PMA alone or coupled with glucose does not modulate intracellular calcium influx [34], [51], [52], [53]. Instead of contributing to
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Experimental conditions may be critical to explain
2021-10-18
Experimental conditions may be critical to explain one model or the other. The matter of Hippo-driven cytoplasmic sequestration (Varelas et al., 2008) of active SMAD complexes (Varelas et al., 2008) vs. TßR basolateral relocalization upon epithelial polarization (Nallet-Staub et al., 2015) as mechan
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MST are involved in signalling pathways following along
2021-10-18
MST1/2 are involved in signalling pathways following along the canonical and noncanonical Hippo pathway. The canonical pathway is highly conserved between D. melanogaster and mammals and a master regulator of tissue growth. During development and within the canonical pathway, MST1/2 seem to have red
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bcl2 br Mechanisms of Resistance As with other cancer treatm
2021-10-18
Mechanisms of Resistance As with other cancer treatments in development, resistance is a concern with HHIs. Most observations regarding HHI resistance originate from patients with BCC [78]. In the clinic, resistance to vismodegib and sonidegib were observed when used to treat advanced BCC [78], [
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Fmoc-Cys(Trt)-ol GPR is present primarily in the pancreas an
2021-10-18
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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Methods br Results br Discussion The current study is the
2021-10-18
Methods Results Discussion The current study is the first to specifically investigate the role of hepatic GPR109A and GPR109B on HDL metabolism and response to niacin therapy. While niacin raises HDL-C levels in humans, it has been reported by others [20], [36] and confirmed by us here that n
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br Materials and methods br
2021-10-18
Materials and methods Acknowledgements The following reagents were obtained through the NIH AIDS Reagent Program, Division of AIDS, NIAID, NIH: SIVagm155-4 from Dr. Vanessa Hirsch and Dr. Philip Johnson; Anti-SIVmac251 Polyclonal; SIVagm tan-1 infectious molecular atp citrate lyase from Drs.
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AFB Fapy dG has been long recognized as
2021-10-18
AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by EMD638683 excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG from s
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br Acknowledgements br Introduction Benzodiazepine BZ treatm
2021-10-18
Acknowledgements Introduction Benzodiazepine (BZ) treatment is widely used for quick and efficient anxiolytic and sedative responses. However, when the use is extended to longer periods, adverse effects emerge. These include tolerance to the initial drug effect, dependence as revealed by withd
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