• During the course of our

  2024-07-16

  

  During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident

• Additional evidence for a putative role of COXs and

  2024-07-16

  

  Additional evidence for a putative role of COXs and 5-LOX in AD derives from pharmacological studies using inhibitors of these enzymes (for review, see Firuzi and Praticò, 2006). In addition to helping delineate the pathobiological mechanisms of AD, these results raise hope for discovering novel the

• Conclusion Twenty compounds with dinitrobenzoate

  2024-07-16

  

  Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5

• We have previously shown that

  2024-07-16

  

  We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific UCB 35625 blockade or activation (Rojas-Corrales et al., 2000). Moreover, i

• br ARIs in the prevention of prostate cancer Prostate

  2024-07-16

  

  5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot

• The first description of autophagy as

  2024-07-16

  

  The first description of autophagy as a tumour suppression process arises from the observation that the initial step regulatory gene, Atg6/BECN1, was monoallelically lost in 40% to 75% of human prostate, breast, and ovarian cancers [31]. However, while BECN1 heterozygous mutant mice develop, with lo

• Zhang et al screened three thousand compounds library

  2024-07-16

  

  Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe

• br Experimental section br Acknowledgements

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  Experimental section Acknowledgements Introduction DJ-1 is a highly conserved, homodimeric protein that was originally cloned as an oncogene capable of transforming AZD6738 sale in cooperation with activated ras[1]. DJ-1 is over-expressed in multiple tumor types and is positively correlated

• br Acknowledgments br Protein microarrays were developed to

  2024-07-16

  

  Acknowledgments Protein microarrays were developed to provide miniaturized high-throughput tools to study protein function, 2'-O-Methyl-ATP australia and post-translational modifications. Just a few years ago, the seminal work performed in Stuart Schreiber's laboratory at Harvard University ()

• br Economics consequences of antibiotic resistance in

  2024-07-16

  

  Economics consequences of antibiotic resistance in a SICU In the era of cost-containment, surgeons also need to consider the economic impact of antibiotic resistance in the surgical patient. Antibiotic-resistant infections are more difficult to treat, are more costly and more likely to be fatal t

• br Experimental section br Acknowledgements This work

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  Experimental section Acknowledgements This work was funded by the Italian Association for Cancer Research (AIRC IG18590 to A.A.), by “Fondi di Ateneo-University of Pisa” years 2009 and 2010 (E. N., S. N., E. O., and A. R.) and partially by the Unipi project P.R.A.2016_27 (E. N., E.O. and A. R.

• Previous studies have thus demonstrated that AR activation g

  2024-07-15

  

  Previous studies have thus demonstrated that AR activation generally correlates with the promotion of urothelial carcinogenesis and cancer growth. In this article, we review available data suggesting their modulation through the AR pathway as well as correlations of AR signals with sensitivity to co

• Liao and van Linden et al

  2024-07-15

  

  Liao [47] and van Linden et al. [48] divided the gap between the N-terminal and C-terminal lobes into a front cleft or pocket, a gate area, and a back cleft. The back pocket corresponds to the gate area and the back cleft. The front cleft includes the Gly-rich loop, the hinge, the linker connecting

• br Liver specific AHR deficiency and energy balance In

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  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

• Notably both circulating adiponectin and

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  Notably, both circulating adiponectin and adipsin were equally diminished by about 50% in Arfrp1 mice consistent with several studies reporting overlapping trafficking routes for their secretion from 3T3-L1 MMP-2 Inhibitor I receptor which was strikingly inhibited upon ablation of TfR-positive endos

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