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Effect of a C C double bond The presence
2020-12-10
Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require
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ARA metabolites which are produced through
2020-12-10
ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic UNC 3230 (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and naturetic in the kidney [14]. On
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CDK lacks DNA binding domains and nuclear localization seque
2020-12-10
CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PAX
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Investigations of mice lacking up to three CDKs
2020-12-10
Investigations of mice lacking up to three CDKs identified the mitosis-regulating kinase CDK1 as the main essential component for the cell cycle, whereas ablation of other 3ma regulators such as CDK2, CDK4, or CDK6 did not result in defective proliferation 12, 13. Mouse models and specific CDK inhi
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Doxycycline HCl australia Among prostaglandins PG PGD remain
2020-12-10
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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br Introduction Al Awqati and his colleagues using R methyli
2020-12-09
Introduction Al Awqati and his colleagues using R(+)-methylindazone, R(+)-[(6,7-dichloro-2-cyclopentyl-2,3-dihydro-2-methyl-1-oxo-1H-inden-5-yl)-oxy] acetic Forskolin (IAA-94) (Landry et al., 1987) isolated the first chloride intracellular ion channel (CLIC) proteins (p64) from bovine kidney cor
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br Materials and methods br Results br Discussion
2020-12-09
Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi
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In this study we reported that over expressed
2020-12-09
In this study, we reported that over-expressed endogenous central ET-1 exerted anti-allodynic and anti-hyperalgesic effects on SNL-induced NP for the first time. Furthermore, we showed that ETA-R mRNA L-817,818 synthesis together with the level of ET-1 was increased in the CNS up to 21days after SN
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Estradiol the predominant circulating estrogen in humans it
2020-12-09
Estradiol, the predominant circulating estrogen in humans, it is mainly secreted by the granulosa cells of the ovarian follicles, and the corpora lutea, by the mechanisms indicated above. On the other hand, estretrol is synthesized exclusively during pregnancy by the fetal liver and reaches maternal
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Introduction Hematopoietic stem cells HSCs in
2020-12-09
Introduction Hematopoietic stem mecamylamine (HSCs) in the adult bone marrow (BM) provide all types of blood cells throughout life, while also self-renewing to maintain blood homeostasis. Blood/marrow stem cell transplantation is the most advanced method to cure patients suffering from hematologica
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ERR is constitutively active in the absence of endogenous
2020-12-09
ERRγ is constitutively active in the absence of endogenous ligand. However, several synthetic ligands that can repress or induce ERRγ function by disrupting ERRγ-coactivator interactions have been reported to date. The estrogen receptor modulators diethylstilbestrol (DES) and 4-hydroxytamoxifen (4-O
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br Acknowledgments br Significance The mechanisms underlying
2020-12-09
Acknowledgments Significance The mechanisms underlying the adverse effects of Epo-stimulating agents on the reduced survival of cancer patients are not well understood. Here, we identified EphB4 as an alternative Epo receptor, which triggers Src/Stat3 signaling via EphB4. We also showed that r
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Here two labs that helped characterize
2020-12-09
Here, two labs that helped characterize these two pathways have worked together to further test whether these apparently parallel pathways from β-AR to CaMKII-RyR might be related in series. Much of the work leading to the Epac pathway involved measurement of Ca sparks as an index of SR Ca leak, oft
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The role of Epac in the regulation of intracellular Ca
2020-12-09
The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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Synthesis of and is described in Scheme Compounds and
2020-12-09
Synthesis of 5–7, 12–14, and 18 is described in Scheme 3. Compounds 5–7 and 18 were prepared as outlined in Scheme 3a. Reaction of 4-bromomethylbenzoic dgat1 inhibitor (36) with thionyl chloride yielded the corresponding acid chloride, which was converted to the corresponding amide 40a by the usual
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