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The anorexic effect observed when AR is infused into the
2024-11-19
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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Later the same group designed and prepared several steroidal
2024-11-19
Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18
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Small kinase inhibitors have been developed to
2024-11-19
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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Autotaxin has been linked to chemoresistance through its abi
2024-11-19
Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer nigericin [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-expressed in patie
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In this paper we describe the
2024-11-19
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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br Innate immune mechanisms that confront viral infection br
2024-11-19
Innate immune mechanisms that confront viral infection Autophagy induction by virus sensing Antiviral xenophagy and virophagy The presence of viral particles within autophagosomal structures has been visualized in only rare instances. This is the case for HSV-1 when it is devoided of ICP34.
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As shown in B the recombinant human LOX nM showed
2024-11-19
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 Lin28 1632 mg and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activities disap
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To circumvent these issues multiple approaches have been dev
2024-11-19
To circumvent these issues, multiple approaches have been developed that target small fractions of the genome, thus reducing the sequencing burden (Dostie et al., 2006; Fullwood et al., 2009; Mumbach et al., 2016). Application of one such approach, chromosome conformation capture carbon copy (5C), w
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These experiments make it clear
2024-11-19
These experiments make it clear that one can study the effect of antimalaria drugs that target the DHFR enzyme of P. falciparum by transferring the malaria enzyme into S. cerevisiae. The ease of growth and manipulation of the yeast make it easy to measure the sensitivity of any particular dhfr allel
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Tetracyclines constitute one of the most important antibioti
2024-11-19
Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200
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br Materials and methods br Results br
2024-11-19
Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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Interestingly we noticed that LPS exposure was associated wi
2024-11-18
Interestingly, we noticed that LPS exposure was associated with decreased phosphorylation of AMPK and increased phosphorylation of p70S6K1, suggesting that AMPK inactivation and the subsequent mTOR activation might be involved in the development of LPS-induced inflammation. On the other side, treatm
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Aerobic exercise plays an important role in the regulation
2024-11-18
Aerobic exercise plays an important role in the regulation of 1,2-Dilauroyl-sn-glycerol receptor metabolism in the skeletal muscle. It is also associated with increases in AMPK and GLUT4 levels, resulting in the improvement of the glucose uptake signaling pathway [17,18]. Recently, it has been show
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br AMPK as a druggable target AMPK signaling has
2024-11-18
AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in
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Similar to Cys Met can undergo ROS
2024-11-18
Similar to Cys, Met can undergo ROS-mediated oxidation to Met sulfoxide, which can result in changes in protein conformation and activity [43]. In our results, the Met content in wild ginseng is higher compared to cultivated ginseng (1.3 times, Table 1). Met is a substrate for the synthesis of vari
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