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br Introduction Androgens have been
2023-03-09
Introduction Androgens have been shown to regulate several neural functions ranging from reproduction to mood and cognitive abilities. This property starts as early as the perinatal period, which is characterized by prenatal and postnatal surges of gonadal testosterone, and continues through pube
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A unique finding in this study is
2023-03-08
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 antibiotics for substrate, can regulate CREB phosphoryation in the context of Alzheimer
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The reactions and the control
2023-03-08
The reactions and the control mechanisms described are all supported by observations. For example the reactions require that different compounds are formed in different groups of AZD2281 cells and this has been observed [15]. Intravenous injection of glycine results in reduced utilisation of glucos
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HT receptors are distributed throughout the brain within
2023-03-08
5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and Kisspeptin 234 (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton
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In this study high concentrations mM of thuringiensin
2023-03-08
In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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Since pyrrolopyrimidine dithiolanes and both displayed parti
2023-03-08
Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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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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