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The product chain length determination mechanism
2022-01-10
The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino smoothened agonist residues in each subfamily of -prenyltransferases have enabled the understanding of the basic
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Reactivation of memory engram neurons underlies memory retri
2022-01-10
Reactivation of memory engram neurons underlies memory retrieval. Neurons activated during memory formation are reactivated during the memory test 24, 25, 32. The reactivation is observed in the cerebral cortex as well as in the hippocampus and amygdala 33, 34. The ratio of the reactivation correlat
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br Neurodystrophic effects of HO It is well known that
2022-01-10
Neurodystrophic effects of HO-1 It is well known that neonatal hyperbilirubinemia (jaundice) may lead to irreversible neurological injury in children (kernicterus). This outcome can be prevented by photodegradation of circulating bilirubin or treatment with metalloporphyrin inhibitors of HO enzym
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br Disp Cleavage and Membrane Trafficking Knowledge of
2022-01-10
Disp Cleavage and Membrane Trafficking Knowledge of how Disp is regulated in Shh-producing lxr agonists to control ligand deployment has, until recently, remained limited. Early studies examining Disp function in Madin–Darby Canine Kidney (MDCK) cells and Drosophila tissue suggested that it is l
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In an attempt to further optimize interactions in
2022-01-10
In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou
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The absence of direct oxidation
2022-01-10
The absence of direct oxidation of Fe2+ by L1 in experiments in solution would be consistent with the recognized low O2 affinity of sGC. It is known that, in bcr-abl tyrosine kinase inhibitors with other hemoproteins, such as globins and heme-containing oxygenases with a Fe2+-proximal histidine link
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MAPK Inhibitor Library The biological activity at GPR a of e
2022-01-10
The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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br Signaling pathways activated by pulsatile GnRH In the
2022-01-10
Signaling pathways activated by pulsatile GnRH In the pituitary, GnRH acts by binding to the G protein-coupled GnRHR on the cell surface of the gonadotrope, inducing interaction of the receptor with heterotrimeric G proteins and catalyzing GTP-GDP exchange on the G protein α subunit (Lambert, 200
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The ester moiety is a promising structural
2022-01-07
The ester moiety is a promising structural motif at the C-3 position for the development of drug-like molecules. However, the labile C-3 ester bond impels these derivate to be susceptible to plasmatic degradation by esterases and this is natural steroidal metabolic process [39,40]. Hence, the isoste
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Tetrazole is one of the most commonly used bioisosteres
2022-01-07
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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GK also called hexokinase IV
2022-01-07
GK, also called hexokinase IV or D, is a glycolytic enzyme that converts brompheniramine maleate to glucose-6-phosphate. GK has unique characteristics compared with those of the ubiquitously expressed hexokinase isoforms I–III, and is predominantly expressed in the pancreas and liver. In pancreatic
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Previous researches about ghrelin focused primarily on
2022-01-07
Previous researches about ghrelin focused primarily on gastrointestinal functions [30], energy balance [31], weight [32], and more recently on anxiety [33], [34], [35] and depression [36]. Here, we provided the first demonstration that chronic peripheral or central ghrelin treatment to CUMS rodents
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br Ghrelin Ghrelin was purified from rat stomach about
2022-01-07
Ghrelin Ghrelin was purified from rat stomach about twenty years ago as a 28-amino 7ACC2 octanoylated peptide and shown to be the endogenous ligand of the growth hormone (GH) secretagogue receptor (now termed GHSR1a, Howard et al., 1996, Kojima et al., 1999). GHSR1a is a 7-transmembrane receptor
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br Acknowledgments We apologize to
2022-01-07
Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Dave Primm (Department of Surgery, University of Texas Southwestern Medical Center) for his critical reading of the manuscript. This work was supported by grants from the US National Institu
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Our previous work demonstrated that KDM regulates cellular o
2022-01-07
Our previous work demonstrated that KDM5 regulates cellular oxidative stress in Drosophila (Liu et al., 2014, Liu and Secombe, 2015). It is known that gut epithelial Rosiglitazone receptor contacted by enteric commensal bacteria generate reactive oxygen species in response to microbial signals (Jone
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