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Ryoichi et al modified potent clinical candidate VX with
2023-07-03
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Introduction Lipoxygenases LOXs are key enzymes that catalyz
2023-07-01
Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic BGB324 (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claesson, 2009).
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Introduction The burden of cardiovascular disease CVD is
2023-06-26
Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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br Acknowledgements This work was supported by
2023-06-15
Acknowledgements This work was supported by the National Key Technology Research and Development Program (2012BAD19B01) and General Financial Grant from the China Postdoctoral Science Foundation (2015M581754). Introduction Cough is one of the most important defensive reflex brought into actio
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Bioactive peptides contain amino acids with possible bioacti
2023-06-15
Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper
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In clinical studies BA has
2023-06-13
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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Imiquimod hydrochloride br ASK in Huntington s disease and o
2023-06-12
ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production
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This study evaluated the anti tumor influences
2023-06-09
This study evaluated the anti-tumor influences of LA against HepG2 Cy5 NHS ester(Et) in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mitochondr
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br Materials and methods br
2023-06-08
Materials and methods Results Discussion Recently, we showed that stimulation of TRPM3 and TRPC6 channels triggers a signaling cascade leading to the activation of AP-1 [11], [12], [13], [15]. The objective of this study was to investigate whether stimulation of TRPV1 channels leads to an a
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Although the immobilization by histidine tag exhibits
2023-06-01
Although the immobilization by histidine tag exhibits effectiveness in oriented enzyme immobilization, it still faces some challenges [31]. On one hand, some unnecessary metal-binding proteins that interfere with the combination between the target protein and the supports or the additional interacti
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Although ACE genetic variance does not
2023-05-30
Although ACE genetic variance does not influence the level of bradykinin significantly, the bradykinin level tends to be affected by ACE inhibitor therapy used by patients. ACE inhibitor reduces the ACE activity that may lead to the accumulation of serum bradykinin. The level of bradykinin tends to
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Sulfo-NHS-Biotin While the direct effects of ARI lead
2023-05-30
While the direct effects of 5-ARI lead to a dramatic Sulfo-NHS-Biotin in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laborator
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To date more than different mutations
2023-05-30
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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The H N mutation in
2023-05-30
The H373N mutation in exon 6 has not previously been reported [3], [4], [5], [6]; thus, this mutation appears to be a novel mutation. The functional expression study demonstrated that the H373N mutation results in almost complete loss of enzymatic activity. Thus, it is highly likely that the H373N m
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scr 11 receptor NOXA a member of the pro apoptotic B
2023-05-30
NOXA, a member of the pro-apoptotic B-cell lymphoma 2 (BCL-2) family, plays a vital role in regulating mitochondrial or inherent apoptotic pathways [7,8]. NOXA binds to MCL-1 with high affinity and interacts with A1 (known as BCL2A1), resulting in BIM release to trigger subsequent apoptosis [9]. In
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