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dpp-4 inhibitor Hinokitiol has versatile abilities as antica
2020-01-20
Hinokitiol has versatile abilities as anticancer, antimicrobial and molecule transport agents and appears to have no developmental toxicity or carcinogenic effects (Imai et al., 2006b). For anticancer activities, it causes apoptosis and dpp-4 inhibitor arrest in many different types of cancers, suc
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Studies carried out with LTRAs before the
2020-01-20
Studies carried out with LTRAs before the identification of the CysLT2R, showed a controversial picture, as results that suggest a role for cysteinyl-LTs in the expansion of ischemic damage and in cardiac dysfunction during reperfusion [5], [68], [69] were evenly balanced by others suggesting that t
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Introduction Collagen deposition is a common feature found
2020-01-19
Introduction Collagen deposition is a common feature found in cancerous tissues and fibrotic organs/lesions. It is now well accepted that collagen deposition is not just a consequence of disease, but that it can also trigger a vicious cycle. Both chemical and physical signals elicited from collagen
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Several CHK inhibitors have been reported in the literature
2020-01-19
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indazo
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Another clinical study indicated the daily
2020-01-19
Another clinical study indicated the daily consumption of green tea with low concentrations of theanine and catechin would improve cognitive function (Ide et al., 2014). Further, in a double blind randomized clinical study involving 102 patients, the Hypericum extract was examined in terms of effica
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Further modifications on the position of compound led to
2020-01-19
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a pow
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Introduction Neuropathic pain occurs in approximately one th
2020-01-17
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) a
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Potential break through technology poised to overcome these
2020-01-17
Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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In mammals NETs contain DNA
2020-01-17
In mammals, NETs contain DNA and antimicrobial proteins composed mainly of nuclear histones, granule-derived neutrophil elastase, myeloperoxidase, lactoferrin, pentraxin, and gelatinase among others [11], [46], [47], [48]. In fish, NETs-like structures have been observed, and DNA staining and immuno
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In accordance with its original discovery EBI
2020-01-17
In accordance with its original discovery, EBI2 may play its major role in response to viral infections or in a pathological context such as in autoimmunity. Although we found a significant delay of onset in the Th17 transfer EAE model, active EAE was unchanged in absence of EBI2. At the moment, we
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Current therapeutic interventions are directed
2020-01-17
Current therapeutic interventions are directed both to prevent (primarily by proper glycemic control) and to treat the advanced stages of diabetic retinopathy, when vision has already been significantly affected. Although these therapies can be very effective in preventing, delaying or reducing visi
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br Introduction As a strong analgesic morphine
2020-01-17
Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft
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br Anti inflammatory effects of MTX In
2020-01-17
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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br Cytokines and NK cells br Combined
2020-01-17
Cytokines and NK cells Combined effects of cytokines and other stimuli on NK cell function Cytokine-stimulated NK 1145 australia have enhanced capacity to kill tumor cells. However, usually, individual cytokines do not seem to be sufficient for full activation, proliferation, survival and eff
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Haggar et al reported the synthesis of
2020-01-17
Haggar et al. reported the synthesis of two new series of 8-(2-imino/oxo/thioxo pyrimidin-4-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 56 (X=O, S, NH) and 8-(pyrazol-3-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 57 [Y=C(O)CH3, 2,4-(NO2)2C6H3]. The 8-acetyl-4-methyl-6-nitro-2-oxo-2
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