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Tamoxifen is included in the treatment
2020-11-11
Tamoxifen is included in the treatment protocol of ER+ breast carcinoma patients routinely. Although tamoxifen improves patients' survival, unfortunately a large number of ER+ patients don't response to tamoxifen treatment (Yager and Davidson, 2006). Detection of molecular markers which could take a
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The compounds were ranked based on the Glide XP
2020-11-11
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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br Materials and methods Male Hartley guinea pigs g
2020-11-11
Materials and methods Male Hartley guinea pigs (300–350g) were obtained from National Laboratory Animal Center, Taiwan. LTD4, LTC4, LTE4, LTB4, montelukast and BAY u9773 were purchased from Cayman Chemical, Ann Arbor, Michigan; Carbachol, atropine, l-serine, boric acid, l-cysteine and all buffer
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br CXCR The CXC receptor and CXCR
2020-11-11
CXCR1/2 The CXC receptor 1 and 2 (CXCR1 and CXCR2) have been well characterised in vertebrates. In mammals and birds, the two receptors are shared by the ELR+ CXC ligands, namely the CXCL8 family members that have proinflammatory roles in recruitment of neutrophils, monocytes and macrophages to s
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br Results and discussion Compounds were
2020-11-11
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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rock br Material and methods br
2020-11-11
Material and methods Results Diagrammatic representations showing the bilateral injection sites in the BNST of all animals used in the present study are presented in Fig. 1. Discussion The present results provide the first evidence that both CRF1 and CRF2 receptors in the BSNT are involved
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br Conclusions br Acknowledgements This work was
2020-11-11
Conclusions Acknowledgements This work was supported by funding from the Natural Sciences and Engineering Research Council of Canada (RGPIN-2017-06346 to JB), National Institute of Child Health and Human Development (5R01HD083930-02 to JB), and the National Institute of Biomedical Imaging and
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System Analysis and Modeling In this work a
2020-11-11
System Analysis and Modeling - In this work, a three-level hierarchical modeling – composed by combinatorial and state-space models – is used: (1) First, failure rates () of TMS servers subsystem units are estimated through continuous Markov chains; (2) Then, the single server dihydrofolate reductas
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Finally considering the encouraging inhibitory and selectivi
2020-11-11
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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Initially studies of GPCRs predominantly assessed the
2020-11-11
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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The selective estrogen receptor modulators
2020-11-11
The selective estrogen receptor modulators (SERMs) are another type of estrogen receptor ligands. The main difference between SERMs and xenoestrogens relies on the fact that SERMs present functional duality and are able to act both as agonists and antagonists of the estrogen receptors in different t
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In order to evaluate the in vivo pharmacology
2020-11-10
In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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Though the physiological roles of microglia derived elastase
2020-11-10
Though the physiological roles of microglia-derived elastases in the CNS are not well understood, their involvement in the metabolism of cholecystokinin [41] and in the processing of plasminogen to produce a low molecular weight plasminogen that enhances neurite outgrowth has been reported [38]. Exp
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Three kinase inhibitors dasatinib type I imatinib type II
2020-11-10
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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br Asb Proteins and Mitochondrial Function Mitochondria are
2020-11-10
Asb Proteins and Mitochondrial Function Mitochondria are intracellular organelles in eukaryotic SB 239063 and are the main sites of oxidative phosphorylation and ATP production. In addition, mitochondria serve as signal transduction docking stations in pyroptosis and regulate a plethora of proce
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