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br Introduction Epidermal growth factor
2020-01-20

Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe
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Our data furthermore suggest that Ch h induced
2020-01-20

Our data furthermore suggest that Ch25h-induced oxysterols could play an important role in modulating the immune cell migration. Mechanistically, we observed impaired trafficking of CD44+CD4+ T cells in mice deficient for Ch25h. CD44+CD4+ T cells lacking EBI2, the receptor of 7α-25OHC, were delayed
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Verapamil a calcium channel blocker used clinically
2020-01-20

Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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In this context we initiated a program to
2020-01-20

In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in cpmt mg replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structural
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br Acknowledgements We thank A Devia Barros and S A
2020-01-20

Acknowledgements We thank A. Devia-Barros and S.A. Barrios Latorre for invaluable technical support during the collection, maintenance and exposure of oysters. We are, furthermore, grateful to the municipal marina of Santa Marta for authorizing access to their facilities and to A. Franco for faci
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Several molecular differences between visceral and subcutane
2020-01-20

Several molecular differences between visceral and subcutaneous adipose tissue have been described. One of the most demarcating differences between adipose depots is the signature of developmental genes, including Hox, Shox, and T-box genes [12], [13]. Lineage tracing studies have revealed key devel
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br Materials and methods br Results br Discussion
2020-01-19

Materials and methods Results Discussion The studies reported here provide a more direct link between conformations of the glycine-rich region of DAPK and enzyme activity. As schematically illustrated in Fig. 3, the various conformations of DAPK with bound substrate or product can be consid
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br Conclusion br Acknowledgements This
2020-01-19

Conclusion Acknowledgements This work is supported by the National Natural Science Foundation of China (41806151, 41706144), the National Natural Science Foundation of China (31330082). We would like to thanks the support of young science and technology talents training fund of South China Agr
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Binding affinity was measured by a
2020-01-19

Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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Both receptors belong to the large family of
2020-01-19

Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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A decrease in heme levels
2020-01-19

A decrease in heme levels enables the phosphorylation of eIF2α by HRI and thereby inhibition of eIF2α activity. Indeed, the relatively small change in cytosolic heme levels in SZ ak7 receptor showed downstream functional consequences manifested by almost 50% elevation in the phosphorylation of eIF2
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br Dienogest DNG Dienogest is a nortestosterone derivative w
2020-01-17

Dienogest (DNG) Dienogest is a 19-nortestosterone derivative with two special structural changes [Fig. 1a]: [a] At the cabon-17 position there is a cyanomethyl group instead of an ethinyl group; [b] A double bond is present between carbons 9 and 10. DNG is the only progestogen that combines prope
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Penciclovir br Introduction Oral contraceptives OCs are
2020-01-17

Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol
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Although PKC in cancer cells is known to promote
2020-01-17

Although PKCδ in cancer 832 582 4016 is known to promote antiapoptotic signaling, a cleaved form of PKCδ, δCF, has been reported to play a contrasting role in enhancing apoptosis (Reyland, 2007), and these complex functions appear to be cell-type dependent (Basu and Pal, 2010). In NSCLC, full-lengt
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br Introduction Addiction to opioids such as morphine is
2020-01-17

Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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