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The G R mutation is
2024-11-29
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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These results validate the docked pose
2024-11-29
These results validate the docked pose of the ALR2-3e complex in comparison to the docked complex of the ALR2-4c complex of which the compound docked completely out of the binding pocket of ALR2 (). This concludes to that the removal of the acetic Cy7 carboxylic acid (non-sulfonated) moiety leads
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The only psychostimulant treatment option in Turkey is
2024-11-29
The only psychostimulant treatment option in Turkey is methylphenidate (Çetin et al., 2015). It is broken down by carboxylase enzyme (CES1) (Sun et al., 2004). From the point of pharmacokinetics, it may be suggested that CES1 gene polymorphisms may be the key responsible factors in patients resistan
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APN accounts for of total plasma proteins
2024-11-29
APN accounts for 0.01% of total plasma proteins in humans; this proportion increases with age to a small extent (Barb et al., 2007). Normal APN levels in the circulation range 3–30μg/mL (Aprahamian and Sam, 2011). APN levels are lower in men than women due to the presence of testosterone and even mo
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br Functional consequences of ADK regulation on astrocyte
2024-11-29
Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in Fludara (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of ADK expressio
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br ACK signaling partners ACK interacts
2024-11-29
ACK1 signaling partners ACK1 interacts with and tyrosine phosphorylates many cellular proteins regulating critical cellular processes [11]. While ACK1 shares common intracellular effectors such as AKT with other signaling pathways, it imparts specificity to signaling by phosphorylating effectors
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Luciferase Immunoprecipitation Systems LIPS which utilizes r
2024-11-29
Luciferase Immunoprecipitation Systems (LIPS), which utilizes recombinant antigens fused to the enzyme reporter Renilla luciferase (Ruc) to detect patient antibodies, provides a unique platform to investigate SP2509 directed against a variety of antigenic targets [25]. Previously, LIPS has been use
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Tacrine an aminoacridine derivative Fig
2024-11-29
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Vortioxetine is a multimodal antidepressant that acts
2024-11-29
Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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In this study in an effort to explore
2024-11-29
In this study, in an effort to explore the possible role of 5-HT6 receptors in mediating the memory-enhancing effects of YL-0919, we first assessed the memory-enhancing effects of YL-0919 in the Morris water maze, object recognition test and step-down passive avoidance task. In addition, we then inv
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Diclazuril During preparation of this manuscript some studie
2024-11-29
During preparation of this manuscript, some studies investigating effects of Sunitinib on Axl activity in renal cancer have been published [44], [45], [46], [47]. However, there are several important considerations to take into account interpreting results of these studies. First, Sunitinib doses th
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As summarized in Fig autophagy
2024-11-29
As summarized in Fig. 1, autophagy up-regulation in terms of Beclin 1 induction, increase of LC3 II and p62 down-regulation were observed between 24 and 72 h of cell incubation, this coinciding with the end of the period 27-OH caused slight reduction of cell viability and proliferation as previously
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NOXA a member of the pro apoptotic
2024-11-29
NOXA, a member of the pro-apoptotic B-cell lymphoma 2 (BCL-2) family, plays a vital role in regulating mitochondrial or inherent apoptotic pathways [7,8]. NOXA binds to MCL-1 with high affinity and interacts with A1 (known as BCL2A1), resulting in BIM release to trigger subsequent apoptosis [9]. In
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Receptor Subtypes and Their Function Critical
2024-11-28
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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br Material and methods br Results br Discussion Asparagine
2024-11-28
Material and methods Results Discussion Asparagine, arginine, leucine, methionine, and glutamine are the essential MK-4827 Racemate for cancer cells and intensively investigated for the development of selective targeted therapeutics. Among them, asparagine depleting bacterial enzyme asparag
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