• This manuscript illustrates the preclinical pharmacological

  2020-07-31

  

  This manuscript illustrates the preclinical pharmacological profile of CR3465 (l-Tyrosine, N-[(2-quinolinyl)carbonyl]-O-(7-fluoro-2-quinolinylmethyl) sodium salt), a new potent and selective leukotriene Cys-LT1 receptor antagonist synthesized by Makovec et al. (2001). CR3465 also has additional anti

• Corticotropin releasing factor CRF is strongly implicated in

  2020-07-31

  

  Corticotropin-releasing factor (CRF) is strongly implicated in negative affect and anxiety states (Radulovic et al., 1999, Takahashi, 2001, Bale and Vale, 2004, Bale, 2005, Lukkes et al., 2009b). Activation of the CRF2 receptors within the serotonergic cell body region, the dorsal raphe nucleus (dRN

• On the basis of the findings described

  2020-07-31

  

  On the basis of the findings described above, a series of heterotricyclic analogs were designed and synthesized. The human CRF1 receptor binding and antagonist activity data for newly designed heterotricyclic core antagonists 28–33 are described in Table 3. Most of the tricyclic core analogs listed

• The selective estrogen receptor modulators SERMs

  2020-07-31

  

  The selective LY500307 receptor modulators (SERMs) are another type of estrogen receptor ligands. The main difference between SERMs and xenoestrogens relies on the fact that SERMs present functional duality and are able to act both as agonists and antagonists of the estrogen receptors in different

• Enolase is of particular interest since it

  2020-07-31

  

  Enolase is of particular interest since it may influence the pathogenic process by three different routes: as a cell surface protein, as a component of the RNA degradosome or as an enzyme. In gram-positive bacteria enolase is found on cell surfaces and binds to laminin, fibronectin, and collagens (a

• br Conclusions br Author contributions br

  2020-07-31

  

  Conclusions Author contributions Introduction The senile plaque, associated with activated microglia and astrocytes, is the pathological hallmark in the brains of patients with Alzheimer\'s disease (AD). Extracellular accumulation of insoluble amyloid-β protein (Aβ) is the main component of

• Although CYP E is also suspected of

  2020-07-31

  

  Although CYP2E1 is also suspected of being the major catalyst of CCl4 reduction in humans [7], the role of the various human CYP450 forms in CCl4 metabolism over a range of CCl4 concentrations has not been established. An understanding of which CYP450 forms contribute to CCl4 metabolism would provid

• Despite advances in our understanding of

  2020-07-31

  

  Despite advances in our understanding of the overall topology of the RING-E2~Ub complex (Dou et al., 2012, Dou et al., 2013, Plechanovova et al., 2012), and the importance of reducing conformational freedom for catalysis (Berndsen et al., 2013), a detailed mechanistic understanding of ubiquitin tran

• br Methods br Results br Discussion Reduced memory capacity

  2020-07-31

  

  Methods Results Discussion Reduced memory capacity is a core cognitive symptom of schizophrenia [2,[4], [5], [6], [7], [8],[11], [12], [13], [14], [15], [16], [17], [18], [19]] and an early marker of ageing-associated cognitive decline [17]. In this study, using a pharmacological approach,

• Numerous studies focused on the mechanisms

  2020-07-31

  

  Numerous studies focused on the mechanisms underlying allosteric changes induced receptor heteromerization and associated modification of downstream signaling but only few reports described roles of endogenous heteromers in vivo (Table 1). This is likely due to limitations of current approaches to d

• The imaging and biochemical data presented here demonstrated

  2020-07-30

  

  The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a

• FOX proteins constitute a large class of transcription facto

  2020-07-30

  

  FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO

• Based on published reports and our own findings we propose

  2020-07-30

  

  Based on published reports and our own findings, we propose to combine genetic inactivation with pharmacological inhibition in mechanistic studies because the selectivity of many commercially available inhibitors is often limited. Experiments with non-selective inhibitors easily lead to misleading c

• In this study Oncomine GEO

  2020-07-29

  

  In this study, Oncomine, GEO and TCGA databases were used to analyze the expression of UBE2S gene in HCC and normal liver tissues to determine the relationship between UBE2S expression and prognosis of hepatocellular carcinoma. The potential function of UBE2S in HCC was analyzed by screening UBE2S c

• RecBCD is a combination helicase nuclease

  2020-07-29

  

  RecBCD is a combination helicase/nuclease that is critical to homologous genetic recombination and DNA repair in E. coli., The holoenzyme consists of the three subunits RecB, RecC, and RecD. The RecB and RecD subunits are NTP hydrolysis-dependent DNA motor proteins that drive DNA translocation and s

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