• A high throughput screening campaign led to the discovery

  2024-11-09

  

  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

• A disruption of lung barrier

  2024-11-09

  

  A disruption of lung barrier function caused by PM2.5 has been observed in our experiments; however the underlying mechanism has not been investigated. Zhao et al. (2018) reported that PM2.5 down-regulated the expression levels of tight junction (TJ) proteins and resulted in nasal epithelial barrier

• br Acknowledgement br Introduction Estrogens play an

  2024-11-09

  

  Acknowledgement Introduction Estrogens play an important role in the development and progression of breast cancer (McGuire et al., 1976; Clemons and Goss, 2001). 17β-Estradiol (E2), the most biologically active estrogen in breast tissue, functions via its nuclear receptors, estrogen receptor (

• The AMP Activated Protein Kinase AMPK has

  2024-11-08

  

  The 5′AMP-Activated Protein Kinase (AMPK) has evolved as an important cellular sensor of reduced energy status that can subsequently phosphorylate its target proteins, slowing the rates of key biosynthetic processes and promoting energy producing pathways; for these reasons AMPK has been proposed as

• Detailed analysis of the dose dependence of A effects

  2024-11-08

  

  Detailed analysis of the dose dependence of Aβ effects revealed that at low amounts, Aβ can also act as a positive regulator of presynaptic activity, enhancing the neurotransmitter release probability and increasing the neuronal excitability [2]. The facilitator effects of low Aβ dose on excitatory

• shows the synthesis of imidazole

  2024-11-08

  

  shows the synthesis of imidazole intermediates , , and . The key precursor keto aldehyde – was prepared in situ by SeO mediated oxidation of corresponding carbonyl compounds and or hydrolysis of dibromo ketone . Subsequent treatment with -Boc piperidine-4-carbaldehyde in the presence of aqueous

• br Liver specific AHR deficiency and energy balance In contr

  2024-11-08

  

  Liver-specific AHR deficiency and energy balance In contrast to the amelioration of hepatic steatosis by global AHR deficiency, targeted knockout of Ahr in hepatocytes exacerbated it in B6 mice fed on a high-fat diet, without interfering with body weight gain [21]. This appeared to result from au

• Additionally regulation of GPCR heteromerization

  2024-11-08

  

  Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut

• Blebbistatin Since forskolin is known to act

  2024-11-08

  

  Since forskolin is known to act directly at the catalytic site of adenylate cyclases near the ATP binding (Tesmer et al., 1997), the synergistic and/or permissive effect of gonadotropins on FSK activity must occur at the level of AC itself or very near, at the level of one of its direct partner. The

• Small RhoGTPases are single domain nucleotide

  2024-11-08

  

  Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine

• Small RhoGTPases are single domain nucleotide

  2024-11-08

  

  Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine

• The purpose of the present study is

  2024-11-08

  

  The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos

• NLX a k a F or befiradol exhibits

  2024-11-08

  

  NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in HBTU to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has show

• In this study we showed that

  2024-11-07

  

  In this study, we showed that TRIM48 promotes ASK1 activation through ubiquitination-dependent degradation of a negative regulator of ASK1 activation, protein arginine methyltransferase 1 (PRMT1). Knocking down TRIM48 suppressed oxidative-stress-induced cell death mediated by ASK1, and the additiona

• Weak and transient interactions of HMGB proteins in such

  2024-11-07

  

  Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o

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