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The phenolic hydroxyl group of
2021-05-11

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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In addition PK studies on indicate that it
2021-05-11

In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted a
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Some studies have been conducted on
2021-05-11

Some studies have been conducted on the activities of CYP450 [[28], [29], [30], [31]]. For example, Chen et al. reported that low-dose aspirin induced the in vivo activity of CYP2C19 in healthy subjects [30], Krasniqi et al. reported that CYP2C8*3 and CYP2C9*2*3 variants correlated with ibuprofen-in
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The two SNPs rs rs
2021-05-10

The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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br Introduction br Conclusion br Acknowledgments and Funding
2021-05-10

Introduction Conclusion Acknowledgments and Funding Introduction Reversible protein phosphorylation is an important post-translational modification of proteins regulating many processes in the cell. Approximately one third of the cellular proteome is phosphorylated, and several sites are
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Previous research has suggested that the acetylcholine
2021-05-10

Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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Raloxifene is a second generation SERM
2021-05-10

Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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br Materials and methods br
2021-05-10

Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic transketolase induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter status
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br Conflicts of interest br Author
2021-05-10

Conflicts of interest Author contributions Acknowledgements This work was supported by the University of Brescia (ex 60%) and Siderurgica Leonessa research funds to AF. RR was supported by Associazione Italiana per la Ricerca sul Cancro - AIRC (MFAG 18459 grant). We are grateful to Umberto
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br Cytokine impact on ILC
2021-05-10

Cytokine impact on ILC fate Increasing evidence shows that ILC2 and ILC3 may convert into ILC1-like PRT062607 Hydrochloride receptor by downregulating either GATA3 or RORγt, respectively, upregulating T-bet and gaining the capacity for IFN-γ production [60,61]. This process, often referred to as
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FOX proteins constitute a large class of transcription facto
2021-05-10

FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO
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Given the important regulatory roles Ub signaling
2021-05-10

Given the important regulatory roles Ub signaling pathways play in eukaryotes, bacterial pathogens and viruses have evolved elaborate mechanisms to hijack host Ub signaling pathways and evade the immune response. This is highlighted by the numerous E3 Ub ligases and spectrum of DUBs encoded by bacte
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Contrary to the profuse dopaminergic
2021-05-10

Contrary to the profuse dopaminergic innervation of the thalamus found in human and non-human primates (Brown et al., 1979, Sanchez-Gonzalez et al., 2005), in rodents, the RTn is one the few thalamic nuclei that receives dopaminergic input (Anaya-Martinez et al., 2006, Garcia-Cabezas et al., 2007, G
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DDR expression is upregulated in the glomeruli and tubules
2021-05-10

DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident Bromosporine is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favo
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We further evaluated the functional relation between promote
2021-05-10

We further evaluated the functional relation between promoter regulation of the tumor suppressor genes and in fresh frozen, microdissected tumor tissue from 55 patient with clear cell renal carcinoma. In addition, normal-appearing tissue from the same patient taken distal of the tumor and later hi
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