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It was recently shown that AHR and
2024-07-12

It was recently shown that AHR and HIF-1α cooperate to support the metabolism of Tr1 brompheniramine maleate receptor [6]. Interestingly, AHR and HIF-1α act sequentially to orchestrate the metabolic remodeling of lymphocytes. While HIF-1α regulates the early metabolic reprogramming of Tr1 cells, AH
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Heart failure is a chronic syndrome in
2024-07-12

Heart failure is a chronic syndrome in which the heart is unable of pumping an adequate supply of blood to meet the metabolic requirements of the body or generating the required elevated ventricular filling pressures to maintain output [34]. Despite considerable advances in the treatment of heart fa
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Obesity is defined as a
2024-07-12

Obesity is defined as a body mass index (BMI) of 30kg/m2 or higher and is known to have a very close association with the risk of developing cancers (Hsueh and Deng, 2016). Several theories exist as to how this link is defined with respect to various cancers, one of which involves the effect of obes
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br Introduction Epilepsy is characterized by spontaneous rec
2024-07-12

Introduction Epilepsy is characterized by spontaneous recurrent seizures and represents one of the most frequent neurological diseases affecting about 60 million people worldwide (McNamara, 1999). It is estimated that up to 50% of all cases are triggered by “initial precipitating injuries”, such
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We found that several anticancer drugs inhibit HT receptor c
2024-07-11

We found that several anticancer drugs inhibit 5-HT3 T 705 current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used frequently t
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The knowledge on the structure of CYP
2024-07-11

The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig
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Small kinase inhibitors have been developed to
2024-07-11

Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha
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br Materials and methods br Results br Discussion The
2024-07-11

Materials and methods Results Discussion The success of CAR-T cell therapy is based on two major facts: one is that cancer cells express tumor-associated antigens (TAAs) on their surface that can be detected by the human immune system; the other is that the CAR molecules target these TAAs o
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death associated protein kinase br Contemporary understandin
2024-07-11

Contemporary understanding for alcoholic cardiomyopathy Up-to-date, a number of theories are postulated for alcoholic cardiomyopathy including generation of mitochondrial reactive oxygen species (ROS), oxidative stress, neurohormonal overactivation (catecholamines and angiotensin II), apoptosis a
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The take home message here is
2024-07-11

The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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Screening a selection of analogues from
2024-07-11

Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to AMG 487 australia 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonst
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As shown in B the recombinant human LOX nM
2024-07-11

As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic Medroxyprogesterone receptor and 5μM DHR. For both purified enzyme and cell lysates, the enzyme a
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Diclofenac The LOX hydroxide metabolites are converted to
2024-07-11

The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4
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Introduction Lipoxygenases LOXs are key enzymes that
2024-07-11

Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic 4-aminopyridine receptor (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells
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Phenolic compounds show reciprocal relationship with
2024-07-11

Phenolic compounds show reciprocal relationship with colonic microflora. Phenolic compounds are able to improve colonic health and modulate microbiota diversity with prebiotic and antimicrobial functions, while colonic bacterial enzymes catalyze deconjugation, dehydroxylation, and convert phenolic c
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