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We further verified the presence of
2019-10-10
We further verified the presence of CLIC1, CLIC4 and CLIC5 in purified mitochondria following protocols described earlier (Singh et al., 2012). As shown in Fig. 4, CLIC4 and CLIC5 were present in the ultra-pure mitochondrial fraction (M3). All the three fractions obtained from 30% (v/v) Percoll grad
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In contrast irinotecan has shown much less myelosuppression
2019-10-10
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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Nrf and HO are key factors in the regulation of
2019-10-10
Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin
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Thus DGK active sites remain ill defined and combined
2019-10-09
Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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Parthenolide and Currently multiple clinical trials of CSF C
2019-10-09
Currently, multiple clinical trials of CSF-1/CSF-1R-targeting agents in combination with standard treatment modalities and immunotherapies are underway (Table 1). In particular, results for combinations with checkpoint blockade inhibitors and other immunotherapeutic approaches are eagerly awaited.
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During the Lapita period in Tonga
2019-10-09
During the Lapita period in Tonga, the Talasiu site would have been an attractive location for human settlement as it overlooked an embayment holding large numbers of sessile and gregarious shellfish close to a fresh water solution channel, with gardening soils immediately inland. However, sea level
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br Non cyclic nucleotide EPAC
2019-10-09
Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2019-10-09
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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Our published results also show
2019-10-09
Our published results also show that the Y2 and the Y5, but not the Y1, receptors mediate NPY-induced excitation-secretion coupling in EECs (Abdel-Samad et al., 2012). Thus, it is highly important to consider controlling ET-1 circulating level via blockade of Y2 and/or Y5 receptor activation (Abdel-
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It was demonstrated that ET signaling is
2019-10-09
It was demonstrated that ET-1 signaling is the primary axon guidance mechanism that accounts for sympathetic innervation of the sinoatrial node and myocardium in the developing mouse heart [11]. In this article, we will review the findings relating to the basic profiles; i.e. molecular features of
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Introduction Cholesterol plays a pivotal role as
2019-10-09
Introduction Cholesterol plays a pivotal role as a constituent of biological membranes and as a precursor for vitamins, hormones and bile acids. Accordingly, its production, distribution, and elimination must be tightly regulated at the cellular and organismal level. Accordingly, dysregulated chole
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Like compound substitution on compound contains amino and
2019-10-09
Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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Prenylation may turn a flavonoid from an agonist to
2019-10-08
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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Of all ES cases approximately are metastatic diseases at dia
2019-10-08
Of all ES cases, approximately 26–28% are metastatic diseases at diagnosis with the remainder being localized disease [14]. Instituting a systemic chemotherapy regimen in combination with surgery and/or radiotherapy has significantly increased the survival of patients with localized disease. The 5-y
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br Materials and methods br Results br Discussion In
2019-10-08
Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel
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