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IC values were obtained for an expanded version
2023-01-29

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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In considering the roles of these enzymes
2023-01-29

In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty CCK Octapeptide, non-sulfated synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes
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Although several different membrane estrogen receptors have
2023-01-29

Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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Apoptosis a major process of programmed cell death and
2023-01-29

Apoptosis, a major process of programmed cell death, and in response to many chemopreventive agents (Jeyamohan et al., 2016). In general, two major signaling pathways control apoptosis, namely, a pathway mediated by cell death receptor and a pathway mediated by mitochondrion, and possible drug targe
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The subnuclear localizations of redox regulators is
2023-01-29

The subnuclear localizations of redox regulators is also largely unknown. The potential role of thiol reductases as transcription regulators or DNA repair molecules may suggest an association to DNA. In this way, the presence of a zinc finger domain potentially involved in protein/DNA interactions o
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br Acknowledgments and Disclosures br Introduction Over the
2023-01-29

Acknowledgments and Disclosures Introduction Over the last decade, the most visible strategy for the treatment of Alzheimer's disease (AD) has been amyloid β peptide (Aβ) immunotherapy (reviewed in [1]). Although the first efforts with Aβ immunotherapy failed to complete clinical trials [1], A
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br MHCI peptide editing N
2023-01-28

MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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shows the synthesis of imidazole intermediates
2023-01-28

shows the synthesis of imidazole intermediates , , and . The key precursor keto aldehyde – was prepared in situ by SeO mediated oxidation of corresponding carbonyl compounds and or hydrolysis of dibromo ketone . Subsequent treatment with -Boc piperidine-4-carbaldehyde in the presence of aqueous NHO
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AI-3 br Rapid nongenomic effects of corticosterone in an am
2023-01-28

Rapid nongenomic effects of corticosterone in an amphibian model Studies in the model organism, the roughskin newt, Taricha granulosa, over 30 years ago led to the discovery that stress can rapidly (within minutes) suppress sexual behavior (amplectic clasping) of male T. granulosa, an effect that
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While HTPCs are not immune cells they produce IL
2023-01-28

While HTPCs are not immune cells, they produce IL-6, MCP-1 and other immunologically relevant factors (Mayer et al., 2016). Our results demonstrated that epinephrine and phenylephrine increased the mRNA expression levels of COX-2, IL-6 and MCP-1 in HTPCs without affecting the mRNA expression level o
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The extent to which GPCR oligomerization
2023-01-28

The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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NLX a k a F or
2023-01-28

NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in bike to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has show
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Sperm total motility and hyperactivated motility
2023-01-28

Sperm total motility and hyperactivated motility are mediated by PLD-dependent protein phosphatase inhibitor polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low mo
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A combination of factors might
2023-01-28

A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to iden
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15-deoxy-Δ-12,14-Prostaglandin J2 In an effort to determine
2023-01-28

In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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