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bacteriological br Conclusion Discovery of an ideal orally
2021-09-26
Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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Thiorphan The FAAH inhibitor activity of the ethoxycarbonyl
2021-09-26
The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound
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br Formation of secretory vesicles and
2021-09-26
Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for tak1 kinase off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Am
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br Materials and methods br Transparency document br Acknowl
2021-09-26
Materials and methods Transparency document Acknowledgments Introduction Hearing loss is the most common congenital sensory deficit. About 1–3 in 1000 children are affected at birth or during early childhood by severe hearing loss, which is defined as prelingual deafness, with at least h
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Through the analysis of various synthetic GPR
2021-09-26
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Necrostatin 1 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discoverin
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Since stroke and cerebrovascular diseases
2021-09-26
Since stroke and cerebrovascular diseases were considered serious AEs following vaccination, we performed manual chart review to confirm the diagnosis and symptom onset date for all stroke and cerebrovascular disease cases identified by ICD-9 codes. Chart review of 131 presumptive cases confirmed 82
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br Material and methods br Results
2021-09-26
Material and methods Results Discussion It is challenging to discriminate between HIV monoinfection and HIV-1/2 dual infection in settings where both viruses co-exist, due to cross-reactivity in serological tests. Thus, the gold standard for detection of HIV-1/2 dual infection is through NA
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Noticeably aminopyrimidine analogs are the most
2021-09-26
Noticeably, aminopyrimidine analogs are the most widely published H4R antagonists and it was Bayer who first disclosed two series of 2-aminopyrimidine compounds possessing significant H4R functional activity. Subsequently, further 2-aminopyrimidine H4R antagonists were published by Pfizer (ZPL-38937
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br Heme and the HO system Heme a
2021-09-26
Heme and the HO system Heme, a complex of iron and protoporphyrin IX, has versatile functions, which are critical for the survival of all aerobic organisms including mammalians and bacteria [9]. The central iron in heme facilitates six ligand binding sites [10], four of which are occupied by nitr
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Following our initial observation of an unexpected increase
2021-09-24
Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present
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GLP is an intestinal peptide hormone that is released
2021-09-24
GLP-1 is an intestinal peptide hormone that is released by the gut following ingestion of food, particularly next and fats. Following its release, GLP-1 stimulates pancreatic β-cells to secrete insulin (Hirasawa et al., 2005, Covington et al., 2006). Originally, GLP-1 acted in a similar manner to g
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br Author contributions br Acknowledgements The work was fin
2021-09-24
Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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br Materials and methods br Results br
2021-09-24
Materials and methods Results Discussion Chronic neuroinflammation underlies the pathogenesis of HAND (Saylor et al., 2016, Sodhi et al., 2004). Infected immune cells release viral proteins and inflammatory factors which act on microglia, astrocytes, and neurons to produce the synaptodendri
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Our experimental results demonstrated http www apexbt com me
2021-09-24
Our experimental results demonstrated marked variability in antioxidant defenses and oxidative damage in Crassostrea gigas between the visceral mass and the gill after the treatments by rifampicin and verapamil through determining the changes of the activity of SOD and POD and MT content. It has bee
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Herein we report the discovery of AM
2021-09-24
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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