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Crystal structures were obtained of
2023-12-16
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Various antiangiogenic drugs have been analyzed over
2023-12-15
Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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br Obstructing SNARE zippering Sharma et
2023-12-15
Obstructing SNARE “zippering” Sharma et al. demonstrated for the first time that in the postmortem AD brains, the level of SNARE complex formation, which is necessary for driving synaptic vesicle fusion at the presynaptic active zone, is significantly reduced [123]. In the absence of changes in e
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br Introduction AMPA receptors AMPARs mediate the
2023-12-15
Introduction AMPA receptors (AMPARs) mediate the majority of fast excitatory postsynaptic currents (EPSCs) in the UO126 receptor (Jonas, 2000). The brevity of EPSCs and rapid deactivation of AMPARs depend upon a short lifetime of synaptically released glutamate, estimated to be about 1 ms (Clemen
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The current guidelines are designed to optimize the detectio
2023-12-15
The current guidelines are designed to optimize the detection of IHC+FISH+ cases, most of which (but not all encountered in our study) being classically good responders to crizotinib therapy (resistance mechanisms to crizotinib therapy were not investigated in our study). In addition to the current
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Dacarbazine receptor Polycyclic aromatic hydrocarbons PAHs a
2023-12-15
Polycyclic aromatic hydrocarbons (PAHs) are abundant environmental contaminants that are produced by the incomplete combustion of organic matter, combustion engines, residential heating, Dacarbazine receptor burning, and industrial activities (Gelboin, 1980; Phillips, 1999, Phillips, 2002). Some PA
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The ARHL locus ahl that
2023-12-15
The ARHL locus (ahl) that contributes to the hearing loss in the C57BL/6J mouse has been mapped to chromosome 10 (Erway et al., 1993, Johnson et al., 1997). It has been shown that strains susceptible to early onset ARHL carry a specific mutation in the cadherin 23 gene (Cdh23), which encodes a compo
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During the course of our
2023-12-15
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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br Experimental procedure br Funding The present
2023-12-15
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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br Introduction Stroke is a
2023-12-15
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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br Autophagy and antiviral innate
2023-12-15
Autophagy and antiviral innate immunity signaling Viral manipulation of autophagy interfering with IFN-I synthesis We have seen that autophagy factors can down-regulate the production of IFN-I induced by RLR engagement during viral infection. In fibroblasts and epithelial cells, there exists c
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br Results br Discussion Both ATM and
2023-12-15
Results Discussion Both ATM and ATR are key regulators of the cellular response to DSBs, yet how exactly they function in concert is not well understood. Recent studies revealed that ATM is required for the resection of DSBs (Jazayeri et al., 2006, Myers and Cortez, 2006), a process necessary
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Tetracyclines constitute one of the most important antibioti
2023-12-14
Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200
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Anti angiogenic activity of natural products in ocular neova
2023-12-14
Anti-angiogenic activity of natural products in ocular neovascularization A number of molecules, obtained from the natural source, have been evaluated for ocular neovascularization [14], [15]. As these compounds exhibit antioxidant effects, these were also tried for their therapeutic efficacy in in
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br Material and methods br Results br Discussion
2023-12-14
Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic CMX001 to support cellular growth and survival. CCH influences the oxygen and glucose supp
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