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HT receptors are distributed throughout the brain within
2024-07-09
5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and Epalrestat (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton et al
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Matrix metalloprotease inhibitors are increasingly available
2024-07-09
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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verapamil hydrochloride br ATX LPA pathway in animal models
2024-07-09
ATX–LPA pathway in animal models of rheumatoid arthritis Several animal models have been used to characterize the mechanisms involved in the pathogenesis of arthritis and to test new therapeutic strategies. The collagen-induced arthritis (CIA) model (Courtenay et al., 1980, Luross and Williams, 2
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Fig summarizes the oxidative metabolism of arachidonic acid
2024-07-08
Fig. 1 summarizes the oxidative metabolism of arachidonic nociceptin receptor by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosino
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The LO has so far only been
2024-07-08
The 15-LO-1 has so far only been found in humans and rabbit reticulocytes [3], [20] and the rabbit 15-LO-1 protein demonstrate 81% identity to the human 15-LO-1. However, rabbit monocytes express an enzyme with mainly 12-LO activity [20], [21]. The high degree of sequence conservation between these
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Apoptosis a major process of programmed cell death
2024-07-08
Apoptosis, a major process of programmed cell death, and in response to many chemopreventive agents (Jeyamohan et al., 2016). In general, two major signaling pathways control apoptosis, namely, a pathway mediated by cell death receptor and a pathway mediated by mitochondrion, and possible drug targe
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There are increasing repeated reports
2024-07-08
There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung
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We report here the first study on
2024-07-08
We report here the first study on the inhibitory effects of the organic nitrates – on human erythrocyte GR. The previous reports by Becker et al., investigated other nitro derivatives (including arylizoalloxazines) by using Beutler’s method, monitoring GR inhibition. Data of show inhibition of hGR
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br Experimental section br Acknowledgements
2024-07-08
Experimental section Acknowledgements The authors thank Prof. Yongbing Cao from School of Pharmacy, the Second Military Medical University, for providing the fluconazole-resistant strains of Candida albicans(strain 100 and strain 103). This work was supported by Program for Innovative Research
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br HIF Blockade in AA Therapy In lieu
2024-07-08
HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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It has been proposed that angiotensin II
2024-07-08
It has been proposed that angiotensin II (Ang II) may upregulate COX-2 expression and the subsequent vasoconstrictor prostanoids production through the activation of AT-1 receptors in vascular smooth muscle cells (Hu et al., 2002). Additionally, this peptide is also able to stimulate the generation
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In the current investigation we studied
2024-07-08
In the current investigation, we studied the effect of propofol on prostate cancer cells. Propofol is one of the most commonly used drugs in the critical care setting and for the induction of general anesthesia and moderate and deep sedation intraoperatively. Recent studies indicated that propofol e
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Afuresertib synthesis Because of the critical roles played
2024-07-08
Because of the critical roles played by AMPK in energy sensing and cancer cell survival, a huge number of drugs have been proposed to exert their pharmacological effects by means of AMPK activation (Kim and He, 2013). For example, metformin has been shown to activate AMPK in muscle (Sajan et al., 20
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Lorlatinib is an orally active brain penetrant
2024-07-08
Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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br Discussion AhR is a receptor that
2024-07-08
Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds
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