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One of pathogenesis of COPD
2022-08-12
One of pathogenesis of COPD is oxidant/antioxidant imbalance. Indeed, it is well known that chronic tobacco smoking is a major risk factor for the development of COPD, and a defect in the detoxification of reactive species produced by cigarette smoke may predispose smokers to airflow obstruction and
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Lactate induced GPR activation was confirmed with a fluorime
2022-08-12
Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within
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Introduction The onset of uterine labor is the
2022-08-12
Introduction The onset of uterine labor is the culmination of a gradual uterine activation wherein physiological inflammation induces a common prolabor pathway characterized by increased myometrial contractility, weakening of fetal membrane integrity, and cervical ripening. Pathological proinflamma
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T L cells can be induced to
2022-08-12
3T3-L1 cells can be induced to differentiate into adipocytes by the appropriate hormonal treatment and they offer a useful in vitro model system for adipogenesis. GPR120 mRNA was detected in differentiated mature adipocytes but not in confluent preadipocytes (Fig. 3A). The level of GPR120 mRNA incre
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Niacin nicotinic acid is widely used to regulate abnormaliti
2022-08-12
Niacin (nicotinic acid) is widely used to regulate abnormalities in plasma lipid and lipoprotein metabolism, as evidenced by its potential for reducing atherosclerotic cardiovascular disease risks (Guyton, 1998), due to its ability to reduce circulating triglycerides and apolipoprotein-B containing
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Flaviviruses consist of a nucleocapsid composed of multiple
2022-08-12
Flaviviruses consist of a nucleocapsid, composed of multiple copies of the capsid protein (C) and the single-stranded, positive-sense RNA genome. The nucleocapsid is surrounded by a lipid bilayer in which two transmembrane proteins are inserted, the envelope glycoprotein E and the membrane protein M
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Epidemiological studies revealed that vitamin D deficiency w
2022-08-12
Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio
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A key limiting factor in the semi
2022-08-12
A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of ubiquitin activating enzyme of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26],
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Receptors for glucagon Gcgr GLP Glp r and
2022-08-12
Receptors for glucagon (Gcgr), GLP-1 (Glp1r), and GLP-2 (Glp2r) are G-protein coupled receptors (GPCRs) belonging to class B-1 (secretin receptor-like) family of GPCRs (Harmar, 2001, Fredriksson et al., 2003). The mammalian Gcgr, Glp1r, and Glp2r genes, together with the osi sc 175 for the receptor
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One effective approach to fine tuning the lipophilicity prof
2022-08-12
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic AICAR phosphate sale scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as w
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Arsenic is generally found in the form of
2022-08-11
Arsenic is generally found in the form of iAs in arsenic plants. Arsenic is primarily metabolized in the liver through methylation processes. Human metabolism of arsenic results in the formation of the methylarsenic metabolites, MMA and DMA, which are more water soluble (Khaleghian et al., 2014; Wei
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br Place in Therapy In the case
2022-08-11
Place in Therapy In the case of minor bleeding, the anticoagulant effects of all FXa inhibitors except betrixaban, which has a longer half-life, will diminish within 24-48 hours of discontinuation of the drug provided the patient has normal renal function. In these cases stopping the FXa inhibito
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br Drug design Over the past decades
2022-08-11
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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The synthesis of substituted pyrimidinone carboxamides is
2022-08-11
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of DCPIB provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford inseparable
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It is apparent from the
2022-08-11
It is apparent from the data in that none of the ligands exhibits significant toxicity as determined by the viability of human embryonic kidney (HEK 293) cells at a concentration of 100 μM. It is also apparent from the data in and that a number of the ligands inhibit the HIV-1 IN enzyme. However, th
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