• We recently employed a functional drug screening approach

  2020-08-26

  

  We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito

• To explore the mechanism behind differential activation kine

  2020-08-26

  

  To explore the mechanism behind differential activation kinetics, Marcott et al. (2018) manipulate local dopamine dynamics. They show that differences in dopamine concentrations are not responsible for different D2R activation kinetics, since D2-IPSCs reach similar amplitudes at different rates in N

• 3-Bromopyruvic acid DNA bound Ku proteins recruit DNA PKcs a

  2020-08-26

  

  DNA-bound Ku proteins recruit DNA-PKcs; and thereby translocate into the duplex by one helical turn, leaving DNA-PKcs near the DNA terminus to assist in tethering the broken ends together [25]. In addition to keeping the DSBs in close proximity, DNA-PKcs may prevent exonucleolytic degradation of the

• Compounds that interact with MDR can do so by

  2020-08-26

  

  Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant auda and there was no observed reduction in

• Proteolysis by CPs is crucially important for cereal seed

  2020-08-25

  

  Proteolysis by CPs is crucially important for cereal seed development and germination. However, these enzymes must be tightly controlled. Pre-harvest sprouting is a phenomenon in which the control of CPs is disrupted. This disruption manifests in the premature synthesis and activation of CPs, leadin

• VEGF inhibition causes vascular regression and

  2020-08-24

  

  VEGF inhibition causes vascular regression and tissue hypoxia in tumor tissues and their surrounding healthy adipose tissues. In this regard, tumors in steatotic livers and adjacent to adipose tissues would experience more hypoxia than non-adipose tumors. Indeed, our present experimental results sup

• chemical library br Discussion Personality develops througho

  2020-08-24

  

  Discussion Personality develops throughout a human\'s life and is related to his or her innate temperament. While personality features are shaped by various experiences of daily life and moderate a wide range of specific behaviours related to particular situational contexts, temperament reveals i

• These findings further extend our knowledge of how P and

  2020-08-24

  

  These findings further extend our knowledge of how P4 and/or E2 can mediate anxiety and fear responses. Female rats in behavioral estrous and ovx rats administered systemic P4 and/or E2 demonstrated significantly less anxiety in the open field and/or elevated plus maze, compared to diestrous rats, a

• We recently employed a functional drug

  2020-08-24

  

  We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito

• br Results br Discussion Adaptive drug

  2020-08-24

  

  Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutat

• A structural explanation for how RBR RING s handle

  2020-08-24

  

  A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon

• br Discussion The regulation of intracellular cholesterol

  2020-08-24

  

  Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec

• Advances in the total chemical

  2020-08-24

  

  Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio

• histamine receptors Enzymatic assay The usual in vitro

  2020-08-24

  

  Enzymatic assay. The usual in vitro test for the measure of the activity of DbH involves ascorbate as a cosubstrate (e.g., 5mM) and tyramine as a substrate (e.g., 10mM). When using N-aryl-N′-hydroxyguanidines instead of ascorbate, the hydroxylase activity of DbH was measured by HPLC as the amounts o

• br Introduction Although not fully understood the

  2020-08-24

  

  Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen

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