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Acknowledgments We are grateful to Dr Jean Marie Bernassau
2020-10-10
Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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There have been two reports of tumor shrinkage in response
2020-10-10
There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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Several of the keloid like lesions
2020-10-10
Several of the keloid-like lesions seen in these individuals were pigmented. It is of potential relevance that genetic variants in DDR1 [MIM: 600408] have been associated with vitiligo, and DDR1 activation is involved when TG101348 sale are attached to collagen-IV fibers. Because DDR1 and DDR2 are
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Previous and ongoing clinical trials have been summarized
2020-10-10
Previous and ongoing clinical trials have been summarized in a recent review (Siaw-Debrah et al., 2017). To our knowledge, there are no ongoing or completed clinical trials focusing on cytokines in ICH. Published studies have focused mainly on cytokine changes in ICH patients (summarized in Table 3)
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The on target in vitro pharmacology of was
2020-10-10
The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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br Methods br Results br Discussion
2020-10-10
Methods Results Discussion On the other hand, surgical patients have to some extent stress during pre- and/or post-operative period. It is well known that CRF/CRF1 receptor is involved in the activation of HPA during acute and chronic stress (Papadimitriou and Priftis, 2009, Zelena et al.,
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In the original ELF study patients were considered
2020-10-10
In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and
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Kim et al reported for bioactive compounds originating
2020-10-10
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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angiotensin ii This study has several limitations First desp
2020-10-10
This study has several limitations. First, despite the relatively large number of participants for a pharmacological neuroimaging study, sample sizes for examining the modulation of THC effects by COMT angiotensin ii were small. Therefore, these particular findings should be interpreted with caution
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ACAT may act as a dimer of dimer
2020-10-09
ACAT1 may act as a dimer of dimer [38]. Within each dimer, it may contain two identical sterol substrate sites (designated as site S), and one or two sterol activator site(s) (designated as site A). Site S preferentially binds pregnenolone (PREG); it can also bind a variety of sterols that contain 3
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The Liver X Receptor and LXRs NR
2020-10-09
The Liver X Receptor-α and -β (LXRs, NR1H3 and NR1H2, respectively) are members of the nuclear receptor superfamily that play a central role in controlling cholesterol homeostasis [9], [10]. In macrophages, LXRs can decrease the cellular sterol burden by inducing expression of the cholesterol efflux
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It is particularly notable that
2020-10-09
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 csf1r in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time and between individ
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Overall the evidence and the
2020-10-09
Overall, the evidence and the results from in vivo studies clearly indicate that cyclosporine biotransformation can be induced by dasatinib co-administration through induction of CYP3A expression. However, further studies are needed to explore the role of P-gp modulation in DDIs. Conclusion In v
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In contrast to inflammatory cytokines TGF has immunosuppress
2020-10-09
In contrast to inflammatory cytokines, TGF-β has immunosuppressive properties yet is also important for tissue imprinting immune cell function during development [23]. Salivary gland (SG) ILCs, in addition to liver and intestinal intraepithelial ILC1, express markers denoting tissue residency and TG
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Primidone CysLTs trigger contractile and inflammatory proces
2020-10-08
CysLTs trigger contractile and inflammatory processes through the specific interaction with cell surface receptors belonging to the rhodopsin family of the G protein-coupled receptor (GPCR) genes. Until now, two receptor subtypes have been cloned, namely CysLT1 and CysLT2[8]. In particular, when th
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