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br Acknowledgment We thank Professor Yuh Chang Sun for
2019-11-30
Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, achi
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2019-11-30
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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From a mechanistic standpoint the BCL
2019-11-30
From a mechanistic standpoint, the BCL6 RD2 domain represses the GPR183 and S1PR1 loci by recruiting HDAC2, but not MTA3-NuRD, to suppress the enhancer activation mark H3K27ac at their distal regulatory elements. However, these data do not exclude the possibility that other as yet unknown corepresso
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The interaction of EPAC with Rim has an important
2019-11-29
The interaction of EPAC2 with Rim1 has an important role in regulating neurotransmitter release. In addition, a recent EPAC2 knockout mice model study provides evidence that EPAC2 promotes transmitter release by maintaining the readily releasable pool (RRP) at mossy fiber (MF) synapses in the hippo
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Similarly synthetic analogs of Alogliptin by replacing the c
2019-11-29
Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in
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Subgroup analysis showed that patients
2019-11-29
Subgroup analysis showed that patients with relatively lower CrCl levels (>50–80 mL/min) were more likely to initiate treatment on a lower dose (17% for all DPP-4 inhibitors; 22% excluding linagliptin). Nevertheless, even in patients with higher CrCl value (>80–120 mL/min and >120 mL/min), at least
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hexamethonium Our results indicate that C CoA
2019-11-29
Our results indicate that C75-CoA is formed in the hypothalamus following stereotaxic injection of C75. Inhibition of hypothalamic CPT1 by C75-CoA in vivo, as seen in our experiments, is independent of the putative inhibition by malonyl-CoA, which may be formed after the action of C75 either on FAS
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Our results showed that in elastase induced AAA TGF neutrali
2019-11-29
Our results showed that in elastase-induced AAA, TGF-β neutralization finely tunes macrophage phenotype. Note that several studies have already addressed the role of M1 markers, such as IL-6 and IL-1β, or M2 markers, including IL-10 and TGF-β.4, 9, 10, 11 The expression and the role of ARG1 in AAA h
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br TRIM TIF A RNF TRIM contains a RING both
2019-11-29
TRIM24 (TIF1A, RNF82) TRIM24 contains a RING-both B-boxes-coiled coil conserved structure at the N-terminus with bromo and PHD domains prior to C-terminal end (Fig. 3). This transcriptional intermediary factor is well studied in the context of transcriptional activation of nuclear receptor via ac
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br Results and discussion br Conclusion Novel and
2019-11-28
Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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The present study sought to determine
2019-11-28
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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Rice approximately covers of land area of the earth
2019-11-28
Rice approximately covers 1% of land area of the earth and it is one of the main sources of food for billions of people [4]. One of the main agriculture industry residues is rice husk, which contains high amount of amorphous silica up to 85–95%. Rice husk ash (RHA) is a solid residue of rice husk co
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Importantly our in vivo data
2019-11-28
Importantly, our in vivo data fit to the in vitro data, further confirming the synergistic effect of XJD and gefitinib on the inhibition of lung cancer and the regulation of SP1, HOTAIR, and EP4 Darifenacin HBr synthesis levels. The doses of XJD used were based on our previous in vivo study (Zhao e
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While showing that deletion of EP maintains femur bone volum
2019-11-28
While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal per
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An important role for the precursor molecule of the
2019-11-28
An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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