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DDR expression is upregulated in the glomeruli and tubules
2021-05-28
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident Deoxynivalenol is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In fav
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Moreover recent structural studies of VEEV nsP pro
2021-05-28
Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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Elevated production of cysLTs in
2021-05-28
Elevated production of cysLTs in DBU receptor and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of particular interest, therefore, t
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In a study on the time course of a
2021-05-28
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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IL is not expressed in tissues constitutively because
2021-05-28
IL-8 is not expressed in tissues constitutively because of its strong chemoattractant, proinflammatory, and angiogenic activities. Rather, it is an inducible factor, produced by a variety of cell types, including leukocytes, fibroblasts, endothelial and epithelial cells, in response to proinflammato
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The phenolic hydroxyl group of ezetimibe tolerated various s
2021-05-27
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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A variety of epidemiological and
2021-05-27
A variety of epidemiological and clinical studies suggest that light alcohol consumption may exert a favorable effects on BP levels but chronic heavy alcohol consumtion causes sustained BP elevation [16], [17]. The hypertensive effect of heavy drinking occurs with all forms of alcohol (i.e. beer win
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In countries such as China where there is a
2021-05-27
In countries such as China where there is a high commercial production of rice, the use of rice husk ash (RHA) as an alternative cementing material can become a great asset for environmental rehabilitation and address the difficult disposal issues associated with this agricultural waste [23]. RHA po
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Several recent reviews have appeared covering different aspe
2021-05-27
Several recent reviews have appeared covering different aspects of the sPLA2 family of enzymes, including sPLA2-V, and the interested reader is kindly directed to these for specific details [34,[135], [136], [137]]. It is important to remark here, however, that recent studies on sPLA2-V suggest that
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A structural explanation for how RBR RING
2021-05-27
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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Acknowledgments br Introduction Diabetes mellitus DM
2021-05-27
Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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Acknowledgments We are grateful to Dr Jean Marie Bernassau f
2021-05-27
Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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Given the excellent in vitro pharmacology profiles of
2021-05-27
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic phenanthroline functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-
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Functional studies suggested the presence of a cysLT recepto
2021-05-26
Functional studies suggested the presence of a cysLT1 receptor. We observed an LTD4-induced cytosolic calcium response, albeit one that was very weak by most standards. The magnitude of the average response was partially explained by the low percentage of ARCA showing a very transient response. Beca
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As described above we designed and synthesized
2021-05-26
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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