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We next determined the selectivity profile of
2022-09-03
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty herpes simplex virus 2 receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affin
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The second patient had a
2022-09-03
The second patient had a homozygous substitution within exon 6 (c.538C>T). The parents were heterozygous and showed no clinical or immunological defect. The mutation has been predicted to alter a potential exonic splicing enhancer (ESE) site. Therefore, exon 6 skipping could be explained by the ESE-
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The strict control of Spi expression
2022-09-03
The strict control of Spi1 expression is critical for proper myeloid cell fate determination, and genetic or epigenetic changes in the Spi1 gene frequently contribute to the leukemogenesis in mice and human. It is has been shown that Spi1 expression is frequently downregulated in human AML patients
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The H autoreceptors distributed mainly
2022-09-03
The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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To interrogate the molecular basis for the myocardial
2022-09-03
To interrogate the molecular basis for the myocardial phenotype in mutant hearts, we performed quantitative real-time PCR (qRT-PCR) expression analysis of genes encoding critical endocardium-derived molecules including Nrg1 and Efnb2. Nrg1 expression was reduced in E13.5 mutant hearts as compared to
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GSK256066 We have previously reported on the effects
2022-09-02
We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t
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A series of P P ureas were explored first
2022-09-02
A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen Eribulin mesylate of the urea yielded , a molecule which retained intrinsic pote
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Several lines of evidence suggest that thermosensation in AF
2022-09-02
Several lines of evidence suggest that thermosensation in AFD is unlikely to be mediated by thermosensitive ion channels. AFD exhibits a steep temperature dependence with a reported Q of >1015 for temperature-evoked current, implying a strong amplification step in the thermotransduction process (Ram
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2022-09-02
Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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The involvement of prostaglandins on the effects induced
2022-09-02
The involvement of prostaglandins on the effects induced by 1-nitro-2-phenylethane is similarly unlikely because vasorelaxation was not changed by indomethacin [20]. The inhibition of adenylyl cyclase with MDL-12330A [21] or cAMP-dependent protein kinase A with KT-5720 [22] also did not interfere wi
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Racemic protein crystallography has been proven to be a powe
2022-09-02
Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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Concerning the molecular mechanisms underlying transcription
2022-09-02
Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1
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br Introduction Nicotinic acid has been used clinically for
2022-09-02
Introduction Nicotinic Nitrotetrazolium Blue chloride has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HD
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br TGR agonists current developments
2022-09-01
TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and 78 9 of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutical industry has
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Taurine sale In addition to gonadotropes GnRHRs have also
2022-09-01
In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa
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