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We are pursuing a hit to lead medicinal
2022-06-30
We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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The haspin gene is also unusual because it lacks
2022-06-30
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 Introduction The signaling molecule nitric oxide NO
2022-06-30
Introduction The signaling molecule nitric oxide (NO) plays an essential role in vessel homeostasis by initiating vasodilation [1], [2], [3]. After biosynthesis in endothelial cells, NO diffuses into the subjacent smooth muscle layer to reach its target enzyme, soluble guanylyl cyclase (sGC, EC
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GSTP is a class Glutathione S transferase GST enzyme
2022-06-29
GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting PLX7904 receptor against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate carcin
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br Author contributions br Conflict of interest br
2022-06-29
Author contributions Conflict of interest Acknowledgments We appreciate technical support of the Research Support Center at the Graduate School of Medical Sciences of the Kyushu University. This study was supported by the Uehara Memorial Foundation and a KAKENHI grant from the Ministry of E
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The pharmacokinetics of was obtained
2022-06-29
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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Research of Kojima et al DeJarnette
2022-06-29
Research of Kojima et al. (2000); DeJarnette et al. (2001), and Saldarriaga et al. (2007) inferred that synchronization of NFWE is related to ovulation response after GnRH-1. In the research of Saldarriaga et al. (2007) with Bos indicus-influenced beef cows, ovulation rate was 40% and estrous synchr
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br Results br Discussion br Materials and Methods
2022-06-29
Results Discussion Materials and Methods Introduction Deoxyribonucleic j 14 synthesis (DNA) is among the most important biopolymers in living organisms alongside carbohydrates and proteins. DNA is a linear polymer consisting of four types of nucleobases, deoxyribose, and phosphate. The
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Introduction l Glutamate is a major excitatory neurotransmit
2022-06-29
Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate i
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Acarbose and voglibose the classic glucosidase inhibitors we
2022-06-29
Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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The effect of the selected compounds on NF kB transrepressio
2022-06-29
The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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Recently unimolecular multi functional peptides that combine
2022-06-29
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with Micafungin and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weigh
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It must be noted that while the accumulated
2022-06-29
It must be noted that while the accumulated evidence on molecular mechanisms has resulted in well-established experimental methods to externally act on single-cell characteristics and networks, safe and efficient external methods to modify multicellular states are still a matter of basic research. C
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Primarily because secretase was a therapeutic target in
2022-06-29
Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in
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Comparison of dlGALRs deduced amino acid
2022-06-29
Comparison of dlGALRs deduced amino tcY-NH2 sequences with that of human GALRs demonstrate that the GALR1 ortholog sequences have diverged less than those of GALR2. Since often duplicate genes undergo divergent evolution through sub-functionalization, loss or gain of new functions (Prince and Picket
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