• The compounds were ranked based on the Glide

  2020-11-26

  

  The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR

• CYP s are heme containing monooxygenases constituting a

  2020-11-26

  

  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

• Deregulated Wnt signaling either due

  2020-11-26

  

  Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen

• R co localizes Golgi marker GM Fig Our metabolic pulse

  2020-11-26

  

  R co-localizes Golgi marker GM130 (Fig. 5). Our metabolic pulse-chase studies carried out in the presence of CSF-1 exposed the newly synthesized CSF-1R to its ligand, which promoted its rapid degradation. While this was clearly seen in control BMDMs, the mature band of CSF-1R remained intact for the

• Based on the ability of CRF to modulate

  2020-11-26

  

  Based on the ability of CRF to modulate nociception, we hypothesized that stress leads to hyperalgesia by the activation of CRF1 and/or CRF2 receptors in the spinal cord. We tested this hypothesis using an acute forced swim as a widely used and easily reproducible stressor and grip force as a measur

• The use of AACSB accreditation as an indicator of expected

  2020-11-26

  

  The use of AACSB accreditation as an indicator of expected performance on the CPA exam has been examined by prior studies (e.g. Barilla et al., 2008, Boone et al., 2006, Grant et al., 2002, Howell and Heshizer, 2006, Lindsay and Campbell, 2003, Marts et al., 1998). While these studies are based on d

• Recent studies showed that the activity of CK was significan

  2020-11-26

  

  Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-

• br Materials and methods br Results and discussion br

  2020-11-26

  

  Materials and methods Results and discussion Conclusions In this study, we have investigated the possibility that hierarchical phosphorylation by CK2 may play a role in cellular signal transduction. Hierarchical phosphorylation by CK2 requires multiple consensus determinants with specific s

• The quantification and monitoring of ChEs enzymatic

  2020-11-26

  

  The quantification and monitoring of ChEs enzymatic activities have traditionally been associated to environmental studies in order to diagnose the exposure of non-target organisms to specific anti-cholinesterasic agents (Nunes, 2011). The importance of these enzymes as biomarkers of environmental c

• br Introduction Estrogens play an important role in the

  2020-11-26

  

  Introduction Estrogens play an important role in the arn 509 (Arevalo et al., 2015). During several decades, estrogen withdrawal in women has been associated with cognitive impairment, increased Alzheimer's disease (AD) risk (Pike, 2017) and with psychiatric disorders such as schizophrenia (Kulk

• We recently employed a functional drug screening approach to

  2020-11-26

  

  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

• Z-YVAD-FMK receptor br Materials and methods br

  2020-11-26

  

  Materials and methods Results Discussion DUSP1 is a member of the subfamily of the Dusl specific phosphatases (DUSPs). High levels of DUSP1 observed in lung, liver and placenta, and low levels have been found in the Z-YVAD-FMK receptor and kidney. DUSP1 has been shown to be elevated in var

• Both progesterone and the calcium ionophore A

  2020-11-26

  

  Both progesterone and the calcium ionophore A23187 rely on the synthesis of cAMP by sAC to elicit exocytosis in human sperm (Fig. 2E-H and [8], [60]). We had reported earlier that digestion of endogenous cAMP with recombinant cAMP-specific phosphodiesterase 4D [9] or inhibition of its synthesis with

• Our observation that nuclear but not cytoplasmic EP expressi

  2020-11-25

  

  Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant TDZD-8 whereas cytoplasmic EP4 was commonly observed [13]. While G protein-coupled recept

• animal Our previous work has demonstrated that two glutamate

  2020-11-25

  

  Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi

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