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br Acknowledgements This work was supported under
2022-04-18
Acknowledgements This work was supported under the National Natural Science Foundation of China (Grant numbers 31200576, 21472197, 21675162), Beijing Natural Science Foundation (Grant No. 7182189), and Project supported by the Joint Funds of the National Natural Science Foundation of China (Grant
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Tail group SAR of the imidazole
2022-04-18
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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Several transgenic and knockout congenic mouse models have
2022-04-18
Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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depicts the synthesis of series with a four step
2022-04-18
depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (–)
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In addition to indoles two additional structural variants we
2022-04-16
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic vps34 side chain to prepare compound (). The extension of the chain was expe
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br Introduction Stroke is the second
2022-04-16
Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A
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When studying the potential of HATi for the treatment
2022-04-16
When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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Relative to the impact of moderate PAE on markers
2022-04-16
Relative to the impact of moderate PAE on markers of histaminergic neurotransmission, there were four salient observations from the studies reported here. First, it does not appear that moderate PAE affects the number of HDC-positive neurons in the tuberomammillary nucleus of the ventral hypothalamu
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br HO and cerebral malaria In a post mortem evaluation
2022-04-16
HO-1 and cerebral malaria In a post-mortem evaluation of human cerebral (falciparum) malaria, strong HO-1 immunostaining was consistently noted in microglia/macrophages within and surrounding the pathognomonic Durck’s granulomas (Schluesener et al., 2001). As witnessed in cerebral trauma specimen
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Sugar gliders and hedgehogs are insectivores
2022-04-16
Sugar gliders and hedgehogs are insectivores and actively seek arthropods in nightly forays. It is suspected that Triatoma were not feeding on the sugar gliders and hedgehogs, but rather were being eaten. The oral route of infection is often nonfatal and induces a carrier state in South American did
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Substrate affinity and specificity can be
2022-04-16
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of e1 ubiquitin bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of s
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The haspin gene is also
2022-04-16
The haspin gene is also unusual because it lacks introns. This is more remarkable when one compares the mammalian genes to those of likely haspin orthologs that are present in the genomic sequences of other species. Such genes in Drosophilamelagonaster, Arabidopsisthaliana and Caenorhabditiselegans
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br Soluble guanylyl cyclase nitric oxide and nitric oxide sy
2022-04-16
Soluble guanylyl cyclase, nitric oxide and nitric oxide synthase The primary and best-studied endogenous activator of soluble guanylyl cyclase (sGC) is nitric oxide (NO), which was originally describe as endothelium-derived relaxing factor for its potent ability to relax blood vessels in response
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Introduction Carbohydrates are some of the most stereochemic
2022-04-16
Introduction Carbohydrates are some of the most stereochemically complex biological molecules found in nature. In addition to their energetic and structural roles in living systems, their role when covalently linked to proteins is critically important in a myriad of molecular recognition processes.
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This work was supported by
2022-04-15
This work was supported by the National Natural Science Foundation of China (Grants 81471101 and 81870852), the Natural Science Foundation of Jiangsu Province (Grant BK20181146), the Natural Science Foundation of the Jiangsu Higher Education Institutions of China (Grants 18KJA320007 and 17KJB320018)
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