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To investigate the mechanism of action of trisubstituted azo
2021-08-13
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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br Materials and methods br Results br
2021-08-13
Materials and methods Results Discussion Adiponectin is one of the most studied adipocytokines. Its release from adipocytes is down-regulated in obesity and other adverse metabolic conditions leading to decreased serum concentrations (Turer and Scherer, 2012). Several factors and conditions
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cathepsin g The proliferation of CCA cell lines
2021-08-13
The proliferation of CCA cell lines can be stimulated by estrogen and other growth factors (Alvaro et al., 2006; DeMorrow, 2009; Mancino et al., 2009). It has also been reported that estrogen positively modulates cholangiocyte proliferation, which is associated with cholangiopathies found in humans
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Although it is well established that
2021-08-13
Although it is well established that estrogen and ESR1 mediate numerous reproductive processes, increasing evidence suggests that ESR2 also lays an integral role in reproduction. ESR2 is a mediator in folliculogenesis and may also act by stimulating ovulation and regulating luteinization (Su et al.,
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br Halogenases Enzymatic C H activation leading to
2021-08-12
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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On the opposite side sPLA
2021-08-12
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer Silydianin and promotes their survival during nutrient stress. It acts through the products of its enzyma
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Because EBI is expressed on the major subsets
2021-08-12
Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile
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ache inhibitors Compounds were synthesized using a facile
2021-08-12
Compounds were synthesized using a facile 8-step convergent synthesis ( and ). Briefly, (Boc)cyclen (compound ) was coupled using TBTU to Fmoc- or Cbz-protected amino alkyl acids (–), followed by deprotection using 20% piperidine in DMF, or H on Pd/C, respectively (–) (). Deprotected linkers were co
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Although the implication of DA and glutamate
2021-08-12
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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Db model cells showed various aberrant phenotypes that seeme
2021-08-12
Db model cells showed various aberrant phenotypes that seemed to reflect the pathological abnormalities found under diabetic conditions. First, in Db model cells after insulin stimulation, we found the inhibition of the transcriptional repression of the gluconeogenic genes, PCK1 and G6PC, and aberra
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br DGAT protein interactions Although DGAT and DGAT are memb
2021-08-12
DGAT-protein interactions Although DGAT1 and DGAT2 are membrane proteins of the ER, the ER contains within its extensive three-dimensional network different, unique structural and functional protein domains that arise from the non-uniformity imposed on it by the intracellular structures it intera
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The present study provides the first evidence that the
2021-08-12
The present study provides the first evidence that the human uroepithelial WEHI-539 hydrochloride in vitro respond directly, within 48h, to this carcinogen by promoting extensive vacuolation and DAPK expression. By using the TEM, ICC and Western blotting, we found that the arsenite-induced vacuoles
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br Introduction Natural killer NK cells have
2021-08-12
Introduction Natural killer (NK) cells have an unique ability to directly lyse transformed, virus-infected or stressed cells without prior sensitization or major histocompatibility complex (MHC) class I restriction [1], [2]. They were initially defined and shown to be important effectors of the i
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Currently it is not known if drought
2021-08-12
Currently, it is not known if drought induces changes in the cysteine protease Santacruzamate A of soybean nodules. The available annotation of the soybean genome, in Phytozome (www.phytozome.net) has identified 706 C1 cysteine protease sequences and 75 C13 cysteine proteases. We have previously re
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br Discussion Our data demonstrate that
2021-08-12
Discussion Our data demonstrate that the bicyclam AMD3100 strongly interacts with CXCR-4, whereas DS and AR177, two other compounds that also interfere with virus entry into the WM-2474 (and interfere with virus binding), do not. AMD3100 is a unique compound in that it interferes with the chemok
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