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br Conclusion Biotransformation of trachyloban oic acid by
2023-03-08
Conclusion Biotransformation of trachyloban-19-oic TAK-632 by S. racemosum provided three products. Oxidation of compound 1 at C-17 (2–3), as well as rearrangement of 1 into a kaurane diterpene hydroxylated in C-16 and C-17 (4) were crucial for increasing AChE inhibitory activity. Compound 3 was
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Although the mechanisms of APP secretion are well characteri
2023-03-08
Although the mechanisms of APP secretion are well characterised (for review see Ref. [1]), production of soluble AChE species is less well understood although we have reported that a metalloproteinase can shed AChE similarly to APP [16], [17]. Recently it has also been demonstrated that cellular pre
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HT modulates cortical and hippocampal pyramidal cell functio
2023-03-07
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal UM171 as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 2015,
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ATX LPA signaling in cancer
2023-03-07
ATX/LPA signaling in cancer is also well known to promote chemotherapy and radiotherapy resistance [7]. Furthermore, others have recently shown that endothelial-derived ATX activity in renal cell carcinoma promotes renal tumorgenesis and acquired resistance to sunitinib through an IL-8-mediated mech
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Aurora A or B selective and pan aurora
2023-03-07
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Aurora A or B selective and pan aurora
2023-03-07
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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IGF is an anabolic growth factor that induces hypertrophy
2023-03-06
IGF1 is an anabolic growth factor that induces hypertrophy and blocks atrophy in skeletal muscle by activating the PI3K/AKT/mTOR pathway (Egerman and Glass, 2014). In addition to its anabolic and anti-catabolic effects, IGF1 stimulates fatty protein kinase g (FA) uptake and glucose metabolism (Clemm
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Transient transfection with ATR kinase dead D A and
2023-03-06
Transient transfection with ATR kinase-dead (D2475→A) [30] and ATM kinase-dead (D2870→Ala and N2875→K) [31] constructs was performed using Fugene 6 (Roche Applied Science, Indianapolis). Three microliters of fugene 6+1μg plasmid was used in transfections using 6-well plates at 2×105 cells/well and a
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SB743921 Two critical determinants of receptor
2023-03-06
Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al
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br Aromatase the key enzyme for estrogen
2023-03-06
Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma
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Coincident with APJ receptor several cell types in the body
2023-03-06
Coincident with APJ receptor, several cell types in the body can synthesize apelin protein. For example, the highest apelin concentrations in the body have been found in the rat central nervous system, pituitary gland, lungs, cardiac muscle, gastrointestinal tract and mammary glands, with lower valu
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A key function of the reference AFST would
2023-03-06
A key function of the reference AFST would be to detect fungal resistance, i.e. to determine which antifungal agents are likely to be clinically inactive [2]. To this end, the epidemiological cut-off value, defined as ‘the upper end of the wild-type (WT) or beginning of the non-wild-type (NWT) MIC d
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Therefore VEGF and its receptors are expressed in different
2023-03-06
Therefore, VEGF and its receptors are expressed in different organs, including the kidneys, the liver and the cki [55]. In the human placenta, VEGF is mainly synthesized by cytotrophoblast and Hofbauer cells early in the first trimester, whereas Flk-1 and Flt-1 receptors are expressed throughout th
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A unique finding in this study is that LO influences
2023-03-06
A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic bay 41 for substrate, can regulate CREB phosphoryation in the context of Alzheimer's di
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LOXs and CYPs are a series of iron containing enzymes
2023-03-06
LOXs and CYPs are a series of iron-containing enzymes that metabolize arachidonic Doxycycline HCl mg to form biologically active products, such as epoxyeicosatrienoic acids (EETs) hydroperoxyeicosatetraenoic acids (HETEs), prostaglandins, leukotrienes and thromboxanes [6]. Among these mediators, 12
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