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In our previous report we synthesized derivatives
2024-02-23
In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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br The future of cancer
2024-02-23
The future of cancer therapeutics with Aurora kinase inhibitors Involvement of Aurora kinases in deregulating multiple tumor suppressor and oncogenic pathways together with the preclinical findings on the efficacy of Aurora kinase inhibitors in attenuating growth of tumor Caspase-6, human recombi
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Aurora A or B selective and pan aurora inhibitors
2024-02-23
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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Nogo-66 (1-40) Demonstration of in vivo efficacy of potentia
2024-02-23
Demonstration of in vivo efficacy of potential chemopreventive agents in animal models is necessary for their clinical development. Our present study provides experimental evidence that CuB 0.1μmol by oral administration (for 2weeks before the cancer cell injection, 5days per week) significantly inh
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br ACL Inhibition Lowering Blood LDL C to Reduce
2024-02-23
ACL Inhibition: Lowering Blood LDL-C to Reduce ASCVD Risk Given its strategic position in the lipid biosynthesis pathway, ACL has been considered an attractive target for lipid-lowering even before statins and their effects on cholesterol homeostasis were elucidated (Box 2). Cells carefully maint
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br Materials and methods br
2024-02-23
Materials and methods Results Dried GSK1016790A used were 48.46 g C. benghalensis, 857.98 g T. zebrina and 25.09 g T. fluminensis. The samples gave 12.9% C. benghalensis, 0.078% T. zebrina and 3.06% T. fluminensis methanol extracts. The methanol extracts were evaluated for their lipoxygenase
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Recent studies have demonstrated significant cross talk betw
2024-02-23
Recent studies have demonstrated significant cross-talk between XRCC1 (a key player in Gefitinib excision repair (BER) and single strand break repair) and DDR [30], [31], [32]. ATM and DNA-PKcs are known to be involved in the phosphorylation of XRCC1 to promote BER [30], [31]. We have recently show
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In Rainey et al published the results
2024-02-23
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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These anatomical studies were followed
2024-02-23
These anatomical studies were followed by the first functional MRI studies of auditory processing in songbirds that were performed in starlings (Van Meir et al., 2005; De Groof et al., 2017; De Groof et al., 2013b) and in zebra finches (Boumans et al., 2008a; Boumans et al., 2007; Boumans et al., 20
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Cy7 NHS ester (non-sulfonated) br Materials and methods br
2024-02-23
Materials and methods Results Discussion Japanese encephalitis caused by JEV is characterized by Cy7 NHS ester (non-sulfonated) neuron death. However, the underlying mechanism is not fully understood. We and other researchers have demonstrated that JEV induces apoptosis by ER stress-mediat
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In receptor binding terminology both
2024-02-22
In receptor binding terminology, both receptor and acceptor contain a receptive site for the ligand, although only the receptor induces a biological function. Moreover, the acceptor lacks an endogenous ligand. Many proteins have been described as receptors for toxic Aβ assemblies, implying a designe
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Introduction Induction of long term potentiation LTP the cel
2024-02-22
Introduction Induction of long-term potentiation (LTP), the cellular correlate of learning and memory, triggers profound changes in the structure and function of excitatory synapses by increasing dendritic spine size and synaptic strength. Significant progress has been made in understanding the int
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It remains to elucidate whether proteolytic activity is
2024-02-22
It remains to elucidate whether proteolytic activity is the cause or the consequence of changing levels of peptidergic substrates. In fact, in some cases, the expression of the enzyme does not necessarily parallel with its activity [26], [55], [57] and other factors such as a definite biochemical en
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In conclusion our study would seem to
2024-02-22
In conclusion, our study would seem to indicate that a hydrophilic microenvironment, which is suitable to accommodate highly hydrophilic molecules with steric hindrance such as aldose hemiacetals, allows the enzyme modulation by one of its most important physiopathological substrates. It is difficul
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br Conflict of interest br Introduction
2024-02-22
Conflict of interest Introduction The Piezo proteins, Piezo1/FAM38A and Piezo2/FAM38B, are multi-pass transmembrane proteins that have been identified as mechanically-activated (MA) homomultimeric, pore-forming ion channels [1,2]. Piezo1 is broadly expressed with its highest expression in blad
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