• The structural similarity software vROCS OpenEye has been ut

  2022-05-26

  

  The structural similarity software vROCS (OpenEye) [45] has been utilized by Musumeci et al. [46] to screen the Maybridge [47] HitFinder database (∼14,400 compounds) using Distamycin A (Fig. 3B) as a query. Using the Tanimoto coefficient (Section 6.4) and vROCS's colour scoring (atom/feature similar

• uPAR promotes cell associated proteolysis by binding to uPA

  2022-05-26

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• Lenvatinib is an orally available multi targeted tyrosine ki

  2022-05-26

  

  Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to

• br Acknowledgements We thank Dr Bhushan Nagar and Dr

  2022-05-26

  

  Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery

• br Anandamide signaling and cardiovascular function The

  2022-05-26

  

  Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate

• Although unexpected based on our predictions low baseline

  2022-05-26

  

  Although unexpected based on our predictions, low baseline and post-stress cortisol being associated with high anxiety has been previously documented in both clinical and healthy populations of humans (Beaton et al., 2006; Jezova et al., 2004; Shirotsuki et al., 2009; Vingerhoets et al., 1996), and

• The haspin gene is also unusual because it

  2022-05-25

  

  The haspin gene is also unusual because it lacks introns. This is more remarkable when one compares the mammalian genes to those of likely haspin orthologs that are present in the genomic sequences of other species. Such genes in Drosophilamelagonaster, Arabidopsisthaliana and Caenorhabditiselegans

• Chronic exposure of cells to cytotoxic

  2022-05-25

  

  Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they

• Aspartame Hypoxia has been shown to affect miR expression

  2022-05-25

  

  Hypoxia has been shown to affect miR-155 expression that can induce autophagy in nasopharyngeal and cervical carcinoma cells [334]. Suppression of miR-155 inhibited hypoxia-induced autophagy. miR-155 targeted mRNAs involved in the PI3K/PTEN/Akt/mTORC1 pathway including: Ras homolog enriched in Aspar

• The opposite modulation observed for circulating LPI levels

  2022-05-25

  

  The opposite modulation observed for circulating LPI levels and WAT GPR55 Erythromycin by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is stimulated. However,

• Several studies have found that GPR possesses a distinct pha

  2022-05-25

  

  Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected HyperScribe Poly (A) Tailing Kit sale expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only

• G protein coupled receptor GPCR

  2022-05-25

  

  G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa

• A considerable body of evidence suggests that alcohols volat

  2022-05-25

  

  A considerable body of evidence suggests that alcohols, volatile anesthetics and inhaled drugs of abuse act at discrete sites on glycine and GABAA receptors, specifically within circumscribed protein pockets (Mascia et al., 2000, Mihic et al., 1997, Beckstead et al., 2000). An amino tolbutamide res

• The standard model of stress postulates

  2022-05-25

  

  The standard model of stress postulates the activation of both the sympathoadrenomedullary axis and the hypothalamo-pituitary-adrenocortical axis. Long-term activation of either neuroendocrine axes has been shown to be harmful [12]. Short-term activation of the sympathoadrenomedullary axis is used t

• Tail group SAR of the imidazole

  2022-05-25

  

  Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl

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