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In vitro studies with soman inhibited non
2024-05-15
In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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The central problem in amnesia
2024-05-15
The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa
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Several dehidropregnenolone derivatives functionalized at C
2024-05-15
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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Finasteride was the first steroidal reductase inhibitor
2024-05-15
Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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br Role of autophagy in
2024-05-15
Role of autophagy in alcoholic cardiomyopathy Concluding remarks The genetic and phenotypic heterogeneity in alcoholic cardiac injury has been recognized despite the seemingly beneficial effects of low to moderate alcohol consumption [8]. Although oxidative stress is well established in the pa
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Aurora A or B selective and
2024-05-15
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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br Conclusion This is the first report to show that
2024-05-15
Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,
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br Extracellular domain architecture The
2024-05-15
Extracellular domain architecture The extracellular region of GABAB receptor exists in a heterodimeric configuration regardless of interactions within the rest of the protein (Geng et al., 2012, Liu et al., 2004, Nomura et al., 2008). The extracellular domains of the GABAB1 and GABAB2 subunits ar
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AP plays a pivotal role
2024-05-15
AP-1 plays a pivotal role in transcriptional regulation of MMP expression. The decoy technique allows the neutralization of AP-1 without any transfection reagents for cellular uptake that cause potential side effects or immune reactions. This energy-dependent transport mechanism of “naked” dODN is c
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br Results Four HT esters butyrate caprylate laurate
2024-05-15
Results Four HT esters (butyrate, caprylate, laurate and stearate esters) were chosen as representative compounds of increasing lipophilicity (Fig. 1). We will refer to them as C4HT, C8HT, C12HT and C18HT, respectively. They have been synthesized, purified and characterized according to our previ
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Recent genome wide association studies have
2024-05-14
Recent genome-wide association studies have indicated SORL1 as a risk factor for AD (Meng et al., 2007, Rogaeva et al., 2007, Wen et al., 2013). SORL1, is expressed in neurons (Yin et al., 2015) and also regulates APP traffic from the cell membrane to the Golgi apparatus. A reduction in its expressi
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br Role of OCT in histamine clearance Histamine is
2024-05-14
Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for
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The rank order of agonist potency in turkey
2024-05-14
The rank order of agonist potency in turkey cardiac chambers demonstrated the predominant presence of the β-adrenergic receptor subtype, in line with the receptor classification by . However, a previous radioligand binding study in the left ventricles of 7-week old turkeys reported the existence of
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ON-01910 australia Mass spectrometry MS analysis and selecti
2024-05-14
Mass spectrometry (MS) analysis and selective enrichment methods of phosphorylated proteins are powerful tools that can help address these challenges. Recent advances in MS have made it possible to analyze signaling pathways by facilitating high-throughput identification of phosphorylation sites wit
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In brief serotonin can interact with
2024-05-14
In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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