• In this study according to the critical pharmacophore T

  2022-06-06

  

  In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested

• Tirapazamine MicroRNAs miRNAs are endogenous small RNA molec

  2022-06-06

  

  MicroRNAs (miRNAs) are endogenous small RNA molecules 20–25 nucleotides in length; they regulate multiple genes by binding to target mRNAs, thereby controlling the stability and translation of protein coding mRNAs (Esteller, 2011, Guo et al., 2010). It has been established that Tirapazamine of the i

• Acknowledgments The authors would like to

  2022-06-06

  

  Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD

• PI-3065 Our results further indicate that low expression of

  2022-06-06

  

  Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi

• Furthermore a direct thiol protective role

  2022-06-05

  

  Furthermore, a direct thiol protective role of S-nitrosylation has been reported in animals [66]. Here, formation of higher order irreversible oxidative modifications, such as sulfinic and sulfonic acids were prevented by S-nitrosylation. All these observations underline the important role of ROS in

• CI994 mg It appears that not all GPR

  2022-06-05

  

  It appears that not all GPR119 agonists require a high dose to elicit acceptable CI994 mg control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitagl

• The compounds described in this paper were prepared using

  2022-06-05

  

  The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m

• Recently a G protein coupled receptor

  2022-06-05

  

  Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Mechanistic studies have suggested that the benefits of niacin therapy may result from the activation of GPR109a located on adipocytes. Recent experiments have shown that niacin activation of GPR109a re

• y15 FPG had no consistent activity

  2022-06-05

  

  FPG-2 had no consistent activity in reducing G→T transversions. Gao and Murphy [2] earlier reported that FPG-2 had a limited amount of activity in vitro on depurinated, UV-treated, and methylene-blue-treated DNA (but not on 8-oxo-G-containing oligonucleotides). FPG-2 contains the N-terminal domain a

• br Acknowledgment br Introduction Positive

  2022-06-05

  

  Acknowledgment Introduction Positive and negative reinforcement are known as the two pivotal components in various models of drug dependence. Compulsive drug seeking behavior results from both the euphoric effects of drug use (positive reinforcement) and the unpleasant withdrawal signs followi

• In this study with the use of C N labeled

  2022-06-05

  

  In this study, with the use of 13C515N2-labeled glutamine, we observed that 13C515N2-labeled glutamine produces a wide range of NAAG isotopologues and its precursors: NAA and glutamate. The NAAG production from glutamine is consistently more elevated in MYC-ON lymphoma and OVCAR4 compared to MYC-OFF

• In agreement with the results obtained from GluR A mice

  2022-06-05

  

  In agreement with the results obtained from GluR-A−/− mice, mice in which the NR1 subunit of the NMDA receptor has been selectively deleted from the CA3 subfield of the hippocampus displayed normal acquisition of the standard reference memory version of the watermaze task (Nakazawa et al., 2002), bu

• br Acknowledgements The authors are grateful for funding pro

  2022-06-05

  

  Acknowledgements The authors are grateful for funding provided by the Health Research Council of New Zealand. Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, fa

• Phylogenetic trees of receptors for

  2022-06-05

  

  Phylogenetic trees of receptors for peptides similar to glucagon from diverse vertebrate species typically are similar to the tree presented in Fig. 3 (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et al., 2005, Cardoso et al., 2006, Ng et al., 2010, Park et al., 2013, Hwa

• Lenvatinib is an orally available multi targeted

  2022-06-02

  

  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

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