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The CRTH inhibitory activities of the
2020-06-11
The CRTH2 inhibitory activities of the synthesized compounds are listed in , . At first we introduced halogen or other substituents at the 4,4′-position of phenyl rings in the benzhydryl moiety in order to obtain SAR and to improve the metabolic stability at this moiety (–). It is well-known that in
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We also identified a role for the transcription
2020-06-11
We also identified a role for the transcription factor p53 in the regulation of the Crm1 promoter. p53 can activate or repress the transcription of target genes. While activation generally occurs through binding of p53 to its consensus binding site in the promoter region of target genes, for example
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Elevated homocysteine has been considered
2020-06-11
Elevated homocysteine has been considered to be a risk factor for vascular dysfunction, vascular disease, and preeclampsia , . The methionine-homocysteine metabolism is responsible for supplying COMT with the methyl-group donor (-adenosyl methionine; SAM) necessary for 2-ME synthesis, and alteration
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na inhibitor br Introduction The cys loop ligand gated ion
2020-06-11
Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri
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Data from immunohistochemical detection of CIC revealed
2020-06-11
Data from immunohistochemical detection of CIC-3 revealed that the immunostaining of CIC-3 can be present both in hepatocarcinoma and its matched normal controls though; CIC-3 was, on the whole, significantly elevated in hepatocarcinoma relative to its paired normal control. In consideration of the
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br Introduction Estrogens play an important role in the
2020-06-11
Introduction Estrogens play an important role in the lactone (Arevalo et al., 2015). During several decades, estrogen withdrawal in women has been associated with cognitive impairment, increased Alzheimer\'s disease (AD) risk (Pike, 2017) and with psychiatric disorders such as schizophrenia (Kulk
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br Menopausal hormone therapy from
2020-06-11
Menopausal hormone therapy, from the beginning to WHI Estrogen products have been used since the 1940s, with increasing prescription through the 1960s. First concerns appeared in the 1970s when oral treatment was linked to uterine cancer. Oral estrogens have traditionally been coupled with proges
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Compound was prepared from chloroindole by acylation to give
2020-06-11
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole Exendin-4 australia derivative (). Derivatives a
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In this study we generated mice in which the
2020-06-11
In this study we generated mice in which the native Bcl6 locus was engineered to produce a form of Bcl6 containing a mutant RD2 domain that disrupts its repressor function. We found that RD2 domain is essential for pre-GC B cell differentiation and clustering into nascent GC within follicles, in par
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Two photon microscopy experiments demonstrated
2020-06-11
Two-photon microscopy experiments demonstrated that most contacts between GC B and Tfh cells are of short duration (about 2 min), and only about 4% of these contacts lead to the formation of stable conjugates (5 to 60 min) (Allen et al., 2007). Similarly, during extrinsic peptide stimulation, some r
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Next we evaluated whether DPP inhibitor suppressed osteoclas
2020-06-11
Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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The photocleaving properties of were studied by
2020-06-11
The photocleaving properties of 1 were studied by performing ΦX174 photocleavage assays. Light irradiation of the mixtures of increasing amounts of 1 with supercoiled DNA caused>90% supercoiled form relaxation and approximately 5% of linearization for the higher concentrations of 1 (1:10bp and 1:2bp
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br Future directions The proposed membrane topology model of
2020-06-11
Future directions The proposed membrane topology model of DGAT1 has only three TMDs, with the N-terminus oriented toward the cytosol and the C-terminus in the ER lumen. The catalytic activity is exclusively on the luminal side of the ER membrane. The second and third TM domains are only about 10
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br Functional significance Defects of the lysyl hydroxylases
2020-06-10
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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Chk and Chk are functionally
2020-06-10
Chk1 and Chk2 are functionally redundant protein kinases that respond to checkpoint signals emanating from the phosphatidylinositol 3-kinase family members ATM (ataxia-telangiectasia mutated) and ATR (Ataxia-telangiectasia and Rad-3 related). A concerted research effort has revealed many mechanistic
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