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Aminothiazole derivatives have been reported to contain anti
2021-03-22

2-Aminothiazole derivatives have been reported to contain antiviral [17], anti-inflammatory [18], and antimicrobial [19] activities. The in vitro anticancer studies showed that different 2-aminothiazole derivatives possess selective and potent inhibitory effect against wide-ranging human cancerous c
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Diabetic retinopathy is a chronic inflammatory
2021-03-22

Diabetic retinopathy is a chronic inflammatory disease. Local inflammation plays a pivotal role in the pathological development and progression of this disease [24]. In addition to TNF-α, several other cytokines, chemokines, and other factors such as IL-1β, IL-6, and C-reactive protein have been ind
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br Materials and methods br Results Artemis has
2021-03-22

Materials and methods Results Artemis has been reported to possess 5′–3′ exonuclease activity in vitro on ssDNA, as well as DNA-PK-dependent endonuclease activity on single-strand overhang and hairpin DNA structures [11]. However, enzymes within the metallo-β-lactamase family typically contain
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Db model cells showed various aberrant phenotypes that seeme
2021-03-22

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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In our current work we have undertaken liquid phase
2021-03-22

In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised hif inhibitor were also screened by molecular docking studies over the reported hDHODH structure. The synthesise
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Dgat mice however had less adipose
2021-03-22

Dgat−/− mice, however, had less adipose tissue, as reflected by lower total fat pad weights and body triglyceride content. Because of these findings, we hypothesized that, although Dgat−/− mice could make triglycerides through non-DGAT pathway(s), their triglyceride synthesis capacity might not be e
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Two nutrient sensing pathways the cAMP
2021-03-22

Two nutrient-sensing pathways, the cAMP-protein kinase A (PKA) pathway and the target of rapamycin complex 1 (TORC1) pathway, are implicated in Msn2/4 regulation. Under non-stress conditions, Msn2 localizes in the cytoplasm and is inactivated by both PKA-dependent phosphorylation of the nuclear loca
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Several TERRA binding proteins have also been discovered
2021-03-22

Several TERRA-binding proteins have also been discovered, especially telomeric duplex DNA binding proteins TRF1 and TRF2, pointing to a significant role of TERRA in more general chromosome biology [14], [20], [21]. TRF2 is a key component of Shelterin that protect chromosome termini [22]. Telomeres
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Phenylbenzofurans are a very important
2021-03-22

Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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Estrogens Definition and history The term estrogens refers t
2021-03-22

Estrogens: Definition and history The term “estrogens” refers to a group of female hormones, including estrone, estradiol, estriol, and estretrol (Fig. 1). Chemically, estrogens belong to the family of organic compounds known as steroids. As such, their core structure is composed of 17 carbon-carbo
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Abdominal aortic aneurysm AAA is considered a major
2021-03-19

Abdominal aortic aneurysm (AAA) is considered a major health concern and is associated with extremely high rates of mortality in case of aortic rupture. The main pathophysiologic mechanisms leading to aortic dilation include the degradation of the extracellular matrix (ECM) components, such as colla
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trifluoperazine synthesis br Rationale and hypothesis To
2021-03-19

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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Like all other cellular processes
2021-03-19

Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con
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In the case of the reaction of a
2021-03-19

In the case of the reaction of 1a with Py2SMeCu(II), compound 4a was observed as the major oxidation product suggesting that further oxidation or hydrolysis of 4a was prevented under our conditions. The precise factors that govern the reactivity and stability of nitrosoamidines remain poorly known.
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ace inhibitors In untreated rodent or human hepatocytes PXR
2021-03-19

In untreated rodent or human hepatocytes, PXR or CAR is stabilized by cytoplasmic co-chaperone partners like heat shock protein 90 (HSP90, Fig. 1). Upon ligand binding, the nuclear receptors are freed and translocated into the nucleus, identified as a pivotal step in PXR- or CAR-mediated transactiva
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