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In this paper we describe the formation of a
2024-07-24

In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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While it is known that
2024-07-24

While it is known that circulating LDL-C levels are largely regulated by either controlling the rate of hepatic production of its triglyceride-rich precursor VLDL particle or the rate of LDLR-mediated LDL particle clearance [58], it should be noted that important differences exist between rodents an
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We also measured macrophage infiltration and CLS
2024-07-24

We also measured macrophage infiltration and CLS presence in peri-gonadal AT from db/db mice and controls. CLS are morphological features within AT that are accurate indicators of adipocyte death and macrophage infiltration [56]. An earlier study showed that CLS macrophages account for >90% of the t
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Thymoquinone TQ is the major
2024-07-24

Thymoquinone (TQ) is the major active Fenofibrate derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al.,
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br Introduction Humans have consumed mushrooms for centuries
2024-07-23

Introduction Humans have consumed mushrooms for centuries because of their high nutrient content and low lipid content, as well as their excellent flavor and texture [1]. Edible mushrooms possess notable medicinal properties and bioactivities, including antitumor, antiviral, antidiabetic, and ant
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HMGA proteins have also been linked to localized changes in
2024-07-23

HMGA proteins have also been linked to localized changes in chromatin/nucleosome structure and alterations of cellular phenotype during induction of gene transcription in activated T lymphocytes. An adaptive immune response is initiated when naïve resting T lymphocytes encounter their corresponding
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br Small molecule homoisoflavonoid in combination
2024-07-23

Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m
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br Conclusion These studies broadly demonstrate that dopamin
2024-07-23

Conclusion These studies broadly demonstrate that dopamine and endocannabinoid signaling in the NAc can have diverse effects on AMPAR-mediated synaptic function depending on previous psychostimulant experience. Here, we examined mechanisms underlying the depotentiation of AMPAR-mediated synaptic
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In this report we introduce a new method
2024-07-23

In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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Ginsenosides are the major bioactive constituents of the Pan
2024-07-23

Ginsenosides are the major bioactive constituents of the Panax ginseng root, which contain many types of ginsenosides including Rb1, Rg1, Rc, and Rg3. The ginsenoside Rb1 appears to be the most abundant of the bioactive ginsenosides [15]. Rb1 exhibits antiinflammatory, anticarcinogenic, and antioxid
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AHR is essential for IL production by T
2024-07-23

AHR is essential for IL-22 production by T NVP-ADW742 and ILC3s [83]. Coexpression of AHR and RORγt by retroviral transduction in a thymoma cell line, EL4, synergistically upregulates IL-22 expression [48]. The cooperativity between AHR and RORγt has also been observed in primary T cells (L.Z., unp
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br Impact of global AHR
2024-07-23

Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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br Introduction Clinical manifestations of Alzheimer
2024-07-23

Introduction Clinical manifestations of Alzheimer's disease (AD) are mainly characterized by progressive intellectual deterioration, memory impairment, cognitive impairment, and psychiatric symptoms. The pathogenesis of AD remains unclear, mainly containing genetic factors, neurotransmitter disor
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Tacrine an aminoacridine derivative Fig A was the first
2024-07-23

Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Matrix metalloprotease inhibitors are increasingly available
2024-07-22

Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi
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