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In humans the superior safety profile of lipid
2024-03-06
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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The increased occurrence of ARIA E in
2024-03-06
The increased occurrence of ARIA-E in APOE ε4 carriers in phase 2 studies resulted in separate protocols for carriers and noncarriers in the subsequent phase 3 studies. Two 18-month trials comprising 1121 carriers and 1331 noncarriers with mild to moderate AD tested doses of bapineuzumab that varied
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Imatinib was first approved for the treatment of Philadelphi
2024-03-06
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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ADOR immunoreactivity was high in
2024-03-06
ADOR immunoreactivity was high in parasympathetically-innervated smooth muscle, namely the iris sphincter muscle and the ciliary muscle. No ADOR immunoreactivity was noted in the sympathetically-innervated iris dilator muscle. Immunoreactivity against all four ADORs was noted in the ciliary epitheli
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Previous studies have demonstrated the presence of soluble N
2024-03-06
Previous studies have demonstrated the presence of soluble NTPDases, 5′-nucleotidase and adenosine deaminase in rat blood serum as well as in human blood (Doleski et al., 2016; Oses et al., 2004; Yegutkin, 1997; Yegutkin et al., 2007). In addition, our earlier reports have shown that these membrane-
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br Results br Discussion To achieve quantitative understandi
2024-03-06
Results Discussion To achieve quantitative understanding of Etoricoxib turnover, we utilize rapidly moving lamellipodial fragments that are geometrically simple, structurally homogeneous, and persistent, and measure relevant rates and concentrations in this system. We find that the lamellipodi
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Very recently Niessen et al have described the resensitizing
2024-03-05
Very recently, Niessen et al. have described the resensitizing effect of MB327 on nAChR performing solid-supported membrane (SSM)-based electrophysiological experiments (Niessen et al., 2016) using plasma membrane preparations obtained from Torpedo californica. These findings validated and underline
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br Discussion Here we focused on seven plant alkaloids
2024-03-05
Discussion Here, we focused on seven plant alkaloids extracted from yokukansan. These alkaloids individually inhibited 5-HT-mediated 5-HT3A and 5-HT3AB receptor currents weakly. Simultaneous administration of these alkaloids, however, inhibited the 5-HT3A and 5-HT3AB receptor currents strongly. T
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The most potent compounds within the current
2024-03-05
The most potent compounds within the current series of compounds were therefore , , , , and , with faah inhibitor possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-
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The knowledge on the structure of CYP including its
2024-03-05
The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig
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aa2414 Using our infection assays we also explored whether l
2024-03-05
Using our infection assays, we also explored whether low-pH compartments were required for the entry of ZIKVs in mammalian cells. Lysosomotropic agents such as ammonium chloride, chloroquine and Bafilomycin A1, strongly inhibited the ability of ZIKVs to enter mammalian cells. Our results are in agre
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Among the most important Ca regulatory
2024-03-05
Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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A third motif involves the toggle switch and
2024-03-05
A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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Based on the results of studies done to
2024-03-05
Based on the results of studies done to-date, there are three characteristics that make a letrozole-based protocol attractive for use in cattle: 1) it is steroid-free, 2) it is cost-effective and requires a shorter time and fewer animal handlings than conventional methods (Table 1), and 3) it may ha
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Introduction The burden of cardiovascular disease CVD is
2024-03-05
Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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