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Over the past decade extensive research
2023-11-30

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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Aurora A or B selective and
2023-11-30

Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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The compounds containing beryllium act
2023-11-30

The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be 7ACC2 []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely strong bidentate Be-bas
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br Conclusion We have identified potential inhibitors of C
2023-11-30

Conclusion We have identified potential inhibitors of C. albicans fungus specific nuclear target outer kinetochore Dam1 complex subunit Ask1, virtually screened through the PubChem compounds database (NCBI, USA) by utilizing state-of-art in silico methods in a pipeline. The 3D protein structure o
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br Experimental Procedures Additional information can be fou
2023-11-30

Experimental Procedures Additional information can be found in Supplemental Experimental Procedures. Author Contributions Acknowledgments We thank all members of Lab of Health Chemistry for helpful discussions. This work was supported by Grant-in-Aid for Scientific Research (KAKENHI) from
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Angiogenesis is a process of
2023-11-29

Angiogenesis is a process of formation of new vessels from arterial vascularization created by endothelial cells. It is essential for the continuous growth of the tumor because it supplies the tumor with nutrients and oxygen, and eliminates cellular waste, which can be toxic to cancer cells [8]. Inf
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br Introduction Sustained over activation of neurohormonal s
2023-11-29

Introduction Sustained over-activation of neurohormonal systems is a hallmark in the pathophysiology of cardiac dysfunction following myocardial infarction (MI) and heart failure (HF). Inhibitors of the renin-angiotensin Levofloxacin mg system (RAAS) constitute cornerstones of pharmacotherapy fo
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Moreover mice exposed to high
2023-11-29

Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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Aldose reductase ALR EC the
2023-11-29

Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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In this study using pure enzyme preparations of human
2023-11-29

In this study, using pure enzyme preparations of human placental recombinant AR (hAR) and of AR isolated from bovine lens (bAR), which behave as Michaelis Mexiletine HCl with glyceraldehyde as substrate, is shown that an apparent negative cooperativity action for glucose still occurs. We present ev
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Cancers that responded to immune checkpoint inhibitors were
2023-11-29

Cancers that responded to immune checkpoint inhibitors were shown to present a type I interferon (IFN) signature in the TME 33, 34. Type I IFNs positively regulate the expression of tumor antigens and their crosspresentation by DCs to tumoricidal CTLs. Furthermore, CD8+ T cell develops full effector
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Small RhoGTPases are single domain nucleotide dependent
2023-11-29

Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine
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Finally one can ask whether these results throw
2023-11-29

Finally, one can ask whether these results throw any light on the nature of the target in SNMG patients. Interestingly, the results of the in vitro incubations suggested that SNMG sera might increase AChR expression to a small extent, raising the possibility that SNMG patients, who have thymic chang
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During the year study period of
2023-11-29

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 Cy5 carboxylic acid (non-sulfonated) of 5.1% for men taking dutasteride (Pe weighed against the prospect of undesirable sexual
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CYP A is one of the key metabolizing enzymes of
2023-11-29

CYP3A4 is one of the key metabolizing Cy5 hydrazide (non-sulfonated) of the cytochrome P450 (CYP) superfamily of heme-containing monooxygenases. As the CYP family of enzymes plays important roles not only in the xenobiotic metabolism and detoxification of a large number of drugs, but also in the bi
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