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The Liver X Receptor and LXRs NR
2020-03-20
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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Loxapine Succinate With respect to bone metabolism
2020-03-20
With respect to ‘bone metabolism and ossification’-related genes, treatment of SaOS-2 osteoblast-like Loxapine Succinate with MS-10 up-regulated IGFBP-4, TG2, and SOST. Up-regulation of IGFBP-4 in SaOS-2 cells inhibits DNA and protein synthesis induced by IGF-1 (Kudo et al., 1995, Kudo et al., 1996
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ion channel Multi subunit RING type E ligases
2020-03-20
Multi-subunit RING-type E3 ligases are exemplified by the CULLIN-RING-ligase (CRL) and the anaphase-promoting complex/cyclosome (APC/C) [19]. CRLs constitute the biggest family of other multi-component E3 ligases. These consist of a cullin scaffold protein (CULLIN 1, 2, 3, 4A, 4B, 5, 7), a substrate
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In the context of E ligase drug discovery
2020-03-20
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 Nif
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In general cellular senescence is considered a programmed re
2020-03-20
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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br Materials and methods br
2020-03-20
Materials and methods Results Discussion The 5-HT2A and D2 receptors have a functional crosstalk (Albizu et al., 2011) and they D-Pantothenic acid are all richly expressed in the mesolimbic and mesocortical systems (Azmitia and Segal, 1978; McMahon et al., 2001), providing the neuroanatomic
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br Acknowledgments br Introduction Heterocyclic chemistry
2020-03-20
Acknowledgments Introduction Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic GSK461364 containing nitrogen and oxygen have shown most potent biological activities. It follo
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br DDR receptor and MMP expression Type II collagen protein
2020-03-20
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrup
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Each nsP plays a distinct defined and indispensable role
2020-03-20
Each nsP plays a distinct, defined and indispensable role in the replication of viral genome. nsP1 is a membrane associated protein which possesses S-adenosyl-L-methionine (SAM)-dependent methyltransferase (MTase) and guanylyltransferase (GTase) activities to catalyze the viral RNA capping reaction
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br Materials and methods br Results br Discussion
2020-03-20
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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Next we evaluated the therapeutic potential of compound
2020-03-20
Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone
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VHb expression in recombinant E coli expressing P H improved
2020-03-20
VHb expression in recombinant E. coli expressing P4H improved Hyp production, presumably by enhancing oxygen transfer. VHb expression contributed to improving growth and extending the period of exponential growth in both shaker flask culture and bioreactor fermentation. A similar phenomenon was also
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Recent pharmacological and clinical studies suggested
2020-03-20
Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and
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FGF ERK signaling has been implicated in
2020-03-20
FGF/ERK signaling has been implicated in epithelial-mesenchymal interactions in a wide range of tissues (Huh et al., 2015, Klein et al., 2006, Rice et al., 2004, Zhang et al., 2006, El Ramy et al., 2005, Volckaert and Langhe, 2015). During embryonic organogenesis and in adult organs, we often observ
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There is an opposite opinion indicating that EphB plays
2020-03-20
There is an opposite opinion indicating that EphB plays a role as cancer suppressor. Batlle et al. showed that loss of EphB expression represented a critical step in CRC progression, and CRCs that lacked EphB2 expression have been correlated with more advanced tumour stage, poor differentiation, and
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