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br Conclusions br Acknowledgments This study was supported
2022-04-09

Conclusions Acknowledgments This study was supported by funds from the National Natural Science Foundation of China (NSFC 31360245, 31460258) and the Applied Basic Research Foundation of Yunnan Province of China (2011FZ111). Introduction Acute myocardial infarction is the undoubted cause o
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In conclusion our work demonstrates for the first time that
2022-04-09

In conclusion, our work demonstrates for the first time that (i) SA-β-gal activity is abundantly present in the gamete cells, such as oocytes and eggs, (ii) the enzyme resides in different cell compartments, (iii) SA-β-gal activity is localized predominantly in acidic endosomal yolk platelets, and (
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Based on the previous report that FXR regulated PEPCK
2022-04-09

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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Statins are recognized by their nephroprotective effect Chmi
2022-04-09

Statins are recognized by their nephroprotective effect (Chmielewski et al., 2002). The hepato- and nephroprotective effects of silymarin are also well studied (Alqasoumi, 2014, Mohamed et al., 2018). Several studies documented increasing Sodium salicylate australia of FXR by statins (Byun et al.,
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Recently a lot of synthetic FFA agonists containing acidic m
2022-04-09

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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Recently they reported an enyne chemotype agonist Fig with
2022-04-09

Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral CT99021 (tmax=15min) and a decent pharmacokinetic profile, a sati
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Endotoxin induced pulmonary hypertension is a reproducible f
2022-04-09

Endotoxin induced-pulmonary Poly (A) Tailing is a reproducible finding in various animal models Leeper-Woodford et al., 1991, Weitzberg et al., 1993 and is also a feature of human sepsis where it may affect right ventricular function (Vincent, 1998). Mechanisms such as vasoconstriction and leukocyt
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Development of few more dihydroxy pyrimidine and N methylpyr
2022-04-09

Development of few more dihydroxy-pyrimidine and N-methylpyrimidone analogues as HIV-integrase inhibitors was attempted involving substitution of variety of five- and six-membered rings via the introduction of a simple methyl substituent in the α-position of the C-2 side chains in order to improve p
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In addition JMJ proteins respond to
2022-04-09

In addition, JMJ proteins respond to biotic stress and abiotic stress in plants. Rice genes OsJMJ704 and OsJMJ705, which have demethylase activities of H3K27me2/3 and H3K4me2/3, respectively, regulate defense-related genes and affect the defense ability of rice against bacterial pathogen Xoo (Li et
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It is important to mention that
2022-04-09

It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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br All platelet agonists acting
2022-04-08

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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Cyclosporin A Having identified initial leads and further le
2022-04-08

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Cyclosporin A derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chlor
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br Material and methods br
2022-04-08

Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing KT182 sale in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involved in the membrane ruf
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Previously we have shown that rapid action of E
2022-04-08

Previously, we have shown that rapid action of E2in vitro is mediated through two E2 membrane receptors, GPR30 (GPER1) and the STX-sensitive membrane receptors (Noel et al., 2008; Kenealy et al., 2011a, Kenealy et al., 2011b). This is significantly different from receptors implicated in the positive
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Armed with this knowledge we looked at ways to reduce
2022-04-08

Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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