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In diseased blood vessels increased production of reactive o
2021-11-15

In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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Compound was synthesized in a racemic
2021-11-15

Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position
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br Introduction High dose niacin or nicotinic
2021-11-15

Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic PP121 form of niacin modulates plasma lipid profiles including decreasing circulating
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Here we performed TEM and AFM imaging to study APE
2021-11-15

Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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Next we investigated the accumulation of H ribavirin in
2021-11-15

Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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br Results and discussion br Conclusion
2021-11-15

Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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br Electron crystallographic structures of connexins The str
2021-11-15

Electron crystallographic structures of connexins The structures of gap junctions are good targets for electron microscopy because they exhibit the characteristic features of self-assembly. Early studies examined the three-dimensional (3D) structures of native gap junction AZD1390 from rodents u
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One effective approach to fine tuning
2021-11-15

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic ARCA EGFP mRNA scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as
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To validate that our natural experiment operates primarily
2021-11-15

To validate that our natural experiment operates primarily through a large negative shock to the risk-taking incentives provided by option compensation measured by vega, we do two sets of tests. First, we confirm a significant drop in vega after the adoption of FAS 123R for treated firms relative to
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br Experimental br Results and discussion
2021-11-15

Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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br STAR Methods br Acknowledgments
2021-11-15

STAR★Methods Acknowledgments We thank the Shanghai Synchrotron Radiation Facility (SSRF) BL18U for help with X-ray data collection. We thank Dr. Thomas F.J. Martin for providing the pcDNA3.1-CAPS-1 plasmid and Dr. Xiaofei Yang for providing the pFHUUIG_shortU6 (l309) plasmid. We thank Dr. Shun
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Parkinson s disease is another neurodegenerative disorder
2021-11-15

Parkinson's disease is another neurodegenerative disorder affecting H3Rs. The most common clinical symptoms of this disease are rigidity, bradykinesia, rest tremor, loss of postural reflexes, and gain impairment owing to progressive degeneration of the dopaminergic neurons in the nigro-striatal neur
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The increased levels of proinflammatory cytokines in BALF
2021-11-15

The increased levels of proinflammatory cytokines in BALF are noted during ALI/ARDS, and the persistent elevation of these mediators may exaggerate systemic or focal inflammatory reaction with a worse outcome. These cytokines, particularly TNF-α and IL-6, play essential roles in ALI [16,17]. The ove
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In the same research group
2021-11-15

In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 an
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GPR has been implicated in
2021-11-12

GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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