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With the nitrogen containing heterocycle
2022-05-05

With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic histone demethylase inhibitor (, and ), followed by deprotection by TFA, smo
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On correlating acute rejection to
2022-05-05

On correlating acute rejection to different risk markers by multiple linear regression analysis, we found that serum FasL and serum creatinine were variables that were independently associated with AR. Carstens et al., reported that significant differences were present between acute rejection and ze
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Data of initial analogs have been
2022-05-05

Data of initial analogs (±)-– have been shown in wherein SAR was observed for the intended change of the right-hand side pyridin-3-yl ring of to various other -containing heteroaryl ring (Ar) disposing the ring- at different directions. Based on consistent human and rat FAAH potency as well as int
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In the next set of experiments we sought
2022-05-05

In the next set of experiments, we sought to determine the source of lysosomal Furosemide synthesis inhibition by oxidative stress. Lysosomal exocytosis probably involves multiple steps including vesicle positioning, delivery, docking and fusion. The previous evidence and data in Fig. 1C,D show that
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br Materials and methods br Results br Discussion
2022-05-04

Materials and methods Results Discussion It was previously shown that heterologous DNA vaccines composed of fused cDNA fragments encoding chimeric NH2-terminal human HER2 and COOH-terminal rat neu sequences stimulated stronger antibody responses and protective antitumor immunity than either
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The molecular mechanisms underlying spindle orientation
2022-05-04

The molecular mechanisms underlying spindle orientation are still largely unknown. Budding yeast has been used to study spindle positioning and asymmetric cell division. Indeed, after cytokinesis, daughter cells have different sizes. The cell division plane is established early in the cell cycle and
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Temozolomide Carbon monoxide another key product from the br
2022-05-04

Carbon monoxide, another key product from the breakdown of heme by HO-1, also plays an important role in the vasculature. Like NO, CO is endogenously derived from the endothelium [68] and can weakly activate sGC by binding to its heme moiety [69]. CO was found to have vasodepressor activity in rats
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br All platelet agonists acting
2022-05-04

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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Spermine NONOate Glutathione transferases GST have been disc
2022-05-04

Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To da
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Waldeck Weiermair et al demonstrated that
2022-05-04

Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp
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Introduction Although G protein coupled receptor GPR
2022-05-04

Introduction Although G-protein-coupled receptor 55 (GPR55) was considered a cannabinoid receptor, it differs phylogenetically from cannabinoid type 1 (CB1) and type 2 (CB2) receptors as it lacks the classic cannabinoid-binding pocket (Baker et al., 2006). GPR55 is sensitive to an array of cannabi
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As part of our discovery efforts searching for
2022-05-04

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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In recent large clinical studies AIM
2022-05-04

In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic nociceptin receptor to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secon
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Stattic mg Molecular properties as well as metabolic
2022-05-04

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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EGTA Over expression of Glo can suppress inflammatory
2022-05-04

Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial EGTA [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen expression
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