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Over the past decade extensive research has been directed
2023-08-23

Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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Jesus et al discovered a new
2023-08-23

Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified Cilomilast 48 and 49 showed IC
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While the yeasts and see Glossary each
2023-08-23

While the yeasts and (see Glossary) each contain only one Aurora homolog, Ipl1p (increase in ploidy 1) and Ark1 (Aurora-related kinase 1), respectively 5, 6, , and Xenopus laevis contain two Aurora kinases: Aurora A and Aurora B [4]. Mammals have three Aurora kinases, A, B, and C (Figure 1). In an
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In clinical studies BA has been reported
2023-08-23

In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani
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In summary this report demonstrates another successful appli
2023-08-23

In summary, this report demonstrates another successful application of gene editing in iPSCs. Despite the lack of efficient metabolic functional repair after transplantation, the application of gene correction into HLCs might still be a realistic goal for ex vivo gene therapy of liver diseases with
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Insulin is the central hormone involved in the control
2023-08-23

Insulin is the central hormone involved in the control of glucose and lipid metabolism. Other nonmetabolic effects of insulin are intensively studied as well. Activation of insulin receptor not only promotes glucose uptake, protein synthesis, and inhibits lipid metabolism, but also is crucial for re
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We have recently begun to demonstrate this
2023-08-23

We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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br Alzheimer s disease AD is an irreversible age associated
2023-08-23

Alzheimer’s disease (AD) is an irreversible, age-associated neurodegenerative disorder that is characterized by progressive memory loss and cognitive decline. AD is also the leading cause of dementia, accounting for 5 million cases in the United States and 44 million cases worldwide. In 2015, AD c
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In large biopsies series from
2023-08-22

In large biopsies series from ALK+ NSCLC treated patients, the number of detected mutations increased after second generation ALKi (Gainor et al., 2016) and in one study were present in 56% of the entire cohort (Shaw et al., 2013b). For example, the rate of G1202R mutations increases from 2% in post
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Mast cells Mast cells are immune cells of the myeloid
2023-08-22

Mast cells. Mast alisertib are immune cells of the myeloid lineage and are ubiquitously present in connective tissues [75]. These cells are involved in the modulation of a number of physiological functions, such as vasodilation, angiogenesis, bacterial, and parasite elimination [75]. Moreover, mast
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br Materials and methods br Results br Discussions Diabetes
2023-08-22

Materials and methods Results Discussions Diabetes is mainly divided into Type 1 diabetes and Type 2 diabetes [16]. Type 2 diabetes, featured by insulin resistance, results from environmental factors and poor eating habits [2]. Type 2 diabetes accounts for more than 95% of the diabetic pati
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During the year study period of men in
2023-08-22

During the 4-year study period, 19.9% of men in the dutasteride group developed prostate cancer as compared to 25.1% in the placebo group, which represents an absolute risk nutlin 3 of 5.1% for men taking dutasteride (Pe weighed against the prospect of undesirable sexual side effects and decreased
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The first natural product described as LO inhibitor
2023-08-22

The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic Rosiglitazone maleate synthesis from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long
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hydrocort br Clinical realities br Commentary on
2023-08-22

Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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IC values were obtained for
2023-08-22

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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