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A high throughput screening campaign led to
2024-12-19
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Mitochondrial dysfunction resulting from mtDNA abnormalities
2024-12-19
Mitochondrial dysfunction resulting from mtDNA abnormalities may trigger retrograde signaling pathways from the mitochondrion to the nucleus, which regulate the expression of genes involved in diverse cellular processes, including metabolism, stress responses, tumor progression, nutrient sensing, li
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TLRs play a key role
2024-12-19
TLRs play a key role in pathogen recognition and early response. In our study, we showed an increase of TLR2 mRNA and protein expression after BMECs were stimulated by S. aureus, as seen for BMECs in a previous study [25]. Although most studies describe TLR4 as a primary receptor for Gram-negative b
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TLRs play a key role
2024-12-19
TLRs play a key role in pathogen recognition and early response. In our study, we showed an increase of TLR2 mRNA and protein expression after BMECs were stimulated by S. aureus, as seen for BMECs in a previous study [25]. Although most studies describe TLR4 as a primary receptor for Gram-negative b
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The basis for the protonation of chitosan is the alkaline
2024-12-19
The basis for the protonation of chitosan is the alkaline primary amino group, which is also the reason for the special properties of chitosan (Guibal, Van Vooren, Dempsey, & Roussy, 2006; Tamer et al., 2017; Yang et al., 2014). Our previous work (Meng et al., 2012) and several other reports (Yan et
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Pathological angiogenesis occurs when an imbalance of endoge
2024-12-19
Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance
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br Funding This study was
2024-12-19
Funding This study was supported by a grant from the Science and Technology Program of Guangzhou (No. 2014Y2-00181) and the personnel training program of Southern Medical University (No. PY2015N023). Conflict of interest statement Authors’contributions Introduction Chronic cerebral hypo
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Based upon these findings the S lipoxygenase
2024-12-19
Based upon these findings, the 12S-lipoxygenase seems to increase membrane excitability by specifically inhibiting M-type K+ channels. The 12S-lipoxygenase is expressed in many parts of mammalian KJ Pyr 9 including the cerebrum, cerebellum, hypothalamus, basal ganglia, hippocampus, olfactory bulb, a
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The mechanism of transformation into SCLC is
2024-12-18
The mechanism of transformation into SCLC is unclear but the loss of retinoblastoma gene (RB) seems important and constitutes an initial event in the tumorigenic process. Some reports revealed the role of the RB gene loss in EGFR mutated NSCLC who transformed into SCLC [15]. In NGS we retrieved mut
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The decreased AR mediated response has
2024-12-18
The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce
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ck1 inhibitor The first rationally designed dual mPGES LO
2024-12-18
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic ck1 inhibitor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synt
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br Regulation of V ATPase assembly
2024-12-18
Regulation of V-ATPase assembly in response to changes in amino 2-Arachidonoyl Glycerol receptor levels A central regulator of cell growth and metabolism is mTORC1 [38]. mTORC1 integrates signals from nutrient availability and growth factor receptors to control such processes as protein and lipi
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In Rainey et al published the
2024-12-18
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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The distribution and subcellular localization differs
2024-12-18
The distribution and subcellular localization differs between the subtypes of mGlu receptors. Most mGlu receptors are broadly expressed in the brain, except for mGlu6, which is restricted to the retina. Some mGlu receptors are additionally found in glial cells, such as mGlu3 and mGlu5 (Aronica et al
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Although several different membrane estrogen receptors have
2024-12-18
Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec