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The manner in which various residue side
2021-12-08
The manner in which various residue side chains are oriented in the active site of HsHxKIV was a driving factor for why glucosamine analogues could not bind, as we previously proposed [16]. These compounds would have difficulty managing access into the active site based on residue P153 in addition t
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br Summary br Acknowledgement br GR A
2021-12-08
Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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The MeO CFO phen yl group was then
2021-12-08
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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In a previous paper we demonstrated immunohistochemically th
2021-12-08
In a previous paper, we demonstrated immunohistochemically the mtep of GHSR-1a in acrosomes and peripheral region of spermatid heads as well as in acrosomes of the spermatids undergoing spermiation [19]. The present study was undertaken to demonstrate the GHSR-1a expression in rat epididymal spermat
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Sickle erythrocytes are known to have an increased adhesion
2021-12-08
Sickle erythrocytes are known to have an increased adhesion to endothelial Pentostatin receptor (Hebbel et al., 1980, Hebbel et al., 1981a, Hebbel et al., 1981b, Wautier et al., 1985, Mohandas and Evans, 1987). Understanding the events associated with vaso-occlusion requires a detailed knowledge of
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FXR agonists represent an attractive class
2021-12-08
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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Based on the previous report that FXR regulated PEPCK indire
2021-12-08
Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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LPCs have been previously described
2021-12-08
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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The second class of proteins necessary
2021-12-07
The second class of proteins necessary for maintaining GSK 2837808A synthesis dynamics is chromatin modifiers, which are considered ‘writers’ and ‘erasers’ and are responsible for modifications of histone N-terminal tails. These post-translational modifications can have direct or indirect effects o
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Liproxstatin-1 br Competing interests br Funding br Ethical
2021-12-07
Competing interests Funding Ethical approval Acknowledgement Introduction Hepatitis C is a disease that infects the liver through transmission of the hepatitis C virus (HCV). Because the symptoms of this infection are not pronounced, the infected individuals may not even be aware of t
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br Biochemical properties and post translational modificatio
2021-12-07
Biochemical properties and post-translational modification of GCAPs GCAPs are hydrophobic proteins that are likely permanently bound to their GC target under physiological conditions [5]. They interact with the photoreceptor GCs through the intracellular domains (reviewed in [17]). GCAP1 has been
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br Rho family GTPases are molecular
2021-12-07
Rho-family GTPases are molecular switches; most which cycle from an ‘on’ GTP bound state to an ‘off’ GDP bound state, driven by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) respectively. Association with lipid membranes through a lipid (farnesyl or geranylgerany
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GnRH ant have been designed
2021-12-07
GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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br Materials and methods br Results br Discussion In
2021-12-07
Materials and methods Results Discussion In this study, the supF forward mutation assay showed that 5OHU induced mutations in human cells and that a C→T mutation was the predominant mutation among 5OHU-induced mutations. In addition, the DNA cleavage activity assay revealed that 5OHU was ex
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It is an aspiring task to apply the glutamate
2021-12-07
It is an aspiring task to apply the glutamate biosensor for in vivo measurements in arn-509 tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in diameter for th
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