• In addition to providing substantial insight

  2020-03-04

  

  In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus

• Our research has demonstrated that the absolute bioavailabil

  2020-03-04

  

  Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin

• A second advance came with the discovery that conformational

  2020-03-04

  

  A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop

• Boulares group has demonstrated that

  2020-03-04

  

  Boulares group [82] has demonstrated that the NF-κB1/p50 NF-κB, a family member of type I NF-κB, is an excellent substrate for DNA-PK, which-dependent phosphorylation of NF-κB1 at serine 20 appears to enhance its binding to DNA as either a homodimer or a heterodimer with p65 NF-κB and the ability of

• Mitochondrial depolarization induced by DHODH inhibition Fig

  2020-03-04

  

  Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ

• Overexpression of EP and DDR has been

  2020-03-04

  

  Overexpression of EP300 and DDR1 has been sporadically reported in the pathogenesis of pulmonary fibrosis and other fibrotic diseases. Zeng et al. reported that EP300 was increased in TGF-β1 treated lung fibroblasts and mediated decreases of SIRT1 expression. Bhattacharyya et al. found that both EP3

• In vitro work by us and others

  2020-03-04

  

  In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan

• CYP s are heme containing monooxygenases constituting a

  2020-03-04

  

  CYP450s are heme-containing monooxygenases constituting a conserved gene superfamily of heme-thiolate proteins, and are found in prokaryotes and eukaryotes (Martignoni et al., 2006). They play a key role in detoxification of endogenous (e.g., steroids) and exogenous compounds (e.g., drug, insecticid

• In S hexyl GSH non

  2020-03-04

  

  In S-hexyl GSH non-treated guinea pigs, antigen-induced anaphylactic response was suppressed by montelukast, but not by BayCysLT2RA, indicating that this asthmatic response was basically CysLT1-receptor-dependent. On the other hand, the suppressive effect of montelukast was weakened by treatment wit

• Recently a sandwich cultured hepatocyte

  2020-03-04

  

  Recently, a sandwich-cultured hepatocyte model has been proved to be a valuable in vitro system that maintains specific hepatic cytomorphology and function relevant to drug metabolism, disposition and toxicity, and thus, closely resembles the in vivo setting. This hepatocyte model was recognized as

• Eukaryotic cell cycle machinery is thought to

  2020-03-04

  

  Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me

• A variety of fused membered ring chemotypes have arisen

  2020-03-04

  

  A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG

• Opiate withdrawal promotes the activation of the corticotrop

  2020-03-04

  

  Opiate withdrawal promotes the activation of the corticotropin-releasing factor (CRF) system, a major coordinator of neuroendocrine and behavioral responses to stressors. For instance, early (8–48 h) morphine withdrawal is associated with increased CRF mRNA expression in the central nucleus of the a

• The CPA EoS was presented by Kontogeorgis

  2020-03-04

  

  The CPA EoS was presented by Kontogeorgis et al., in 1996 [23]. The proposed equation is composed of two parts (SRK EOS + association term) such that it can well predict the thermodynamic behavior of hydrogen bonding materials as a result of considering the association term. Yakoumis et al. (1997) e

• Self Determination Theory SDT as described by Ryan and Deci

  2020-03-04

  

  Self-Determination Theory (SDT), as described by Ryan and Deci (2000) is “an approach to human motivation and personality that uses traditional empirical methods while employing an organismic metatheory highlighting the importance of humans\' evolved inner resources for personality development and b

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