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Because of the commercial availability of some
2022-03-18

Because of the commercial availability of some acetamide phenol starting materials, a few acetamide final products (such as and , ) were directly synthesized via a Mitsunobu reaction with chloropyrimidine piperidinyl cyclopropyl alcohol . The 3-pyridinyl analogue was synthesized by a nucleophilic
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We also observed a significantly higher
2022-03-18

We also observed a significantly higher SLC10A1 gene expression and NTCP protein level among metastatic individuals vs. donor livers. Na+/taurocholate co-transporting polypeptide (NTCP), which is expressed on the basolateral membrane of hepatocytes and is primarily responsible for the uptake of bile
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In contrast to short term
2022-03-18

In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty tandospirone oxidation cycle [13], decreased NADPH content [14], endoplasmic reticulum (ER) st
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Epinephrine responses to hypoglycemia are probably triggered
2022-03-17

Epinephrine responses to hypoglycemia are probably triggered centrally, perhaps with input from peripheral hypoglycemia sensing [3], [4]. We observed increased epinephrine responses in GCK-MODY and I366F diabetic mice. Consistent with a role for full-time job GCK in detecting a low blood glucose, w
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2'-O-Methyl-ATP br Acknowledgments This work was funded
2022-03-17

Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa
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Prior to proceeding to the
2022-03-17

Prior to proceeding to the main tests, essential conditions were optimized. At first, we tested whether the parameters that were successful in inducing LacZ gene for the production of β-galactosidase enzymes in E. coli culture system in our previous study would be sufficient to induce LacZ gene in t
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The snapshots in Fig were taken at the end
2022-03-17

The snapshots in Fig. 5 were taken at the end of the first platteau i.e. for 5 Å rmsd or 4 ns time. Thus, we can see that the state of the i-motif affects the mechanism of the G-quadruplex unfolding. At acidic pH the stiff structure of the i-motif does not affect the bottom part (the innermost) of t
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br Melanoma cell lines There is suggestive epidemiological e
2022-03-17

Melanoma cell lines There is suggestive epidemiological evidence that omega-3 PUFA can be preventative against melanoma, although the mechanisms of this relationship has not been extensively investigated [65], [66]. A 2014 study demonstrated that DHA inhibited cell proliferation in vitro in A2058
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Recently some researchers working in China Pharmaceutical Un
2022-03-17

Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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Conclusions br Author information The
2022-03-17

Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu
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It is considered that activations of MMP and MMP are
2022-03-17

It is considered that activations of MMP-2 and MMP-9 are closely related to progression process of cancer cells, such as invasion and metastasis [22], [23]. In fibrosarcoma cells, GPR40 suppressed not only MMP-2 and MMP-9 activations, but also cell motile and invasive activities, suggesting GPR40 ne
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Preliminary explorations focused on the linker of Table
2022-03-17

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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The Rho family of GTPases is composed of many
2022-03-17

The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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br Acknowledgments R Dalmann has obtained a bourse
2022-03-17

Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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Despite a large amount of uptake for both
2022-03-17

Despite a large amount of uptake for both nanoparticles, only after transport across intestinal epithelia do the nanoparticles really contribute to improving absorption. Though the transport of nanorods across monolayer was a little bit more than nanospheres, the total transport was less than 2% (A1
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