• EBI remains an orphan GPCR

  2020-10-09

  

  EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et

• br Discussion and conclusion Ubiquitination and deubiquitina

  2020-10-09

  

  Discussion and conclusion Ubiquitination and deubiquitination have emerged as important mechanisms involved in p53 management. This review revealed that various DUBs can regulate p53 or p53-Mdm2-MdmX networks. Herein, we reviewed the current progress made toward elucidating the complexities in th

• Impaired dopaminergic systems associated with MA have

  2020-10-09

  

  Impaired dopaminergic systems associated with MA have been well-documented (Walsh and Wagner, 1992, Kim et al., 1999, Nakajima et al., 2004, Shin et al., 2012, Shin et al., 2017b, Dang et al., 2016, Dang et al., 2017b). Previous reports have suggested that early MA use may be linked to higher risk f

• Protein expression and purification A mL overnight culture o

  2020-10-09

  

  Protein expression and purification. A 3 mL overnight culture of E. coli BL21 (DE3) pLysS pGEX-6P-3-A1S_0222 was grown in Luria-Bertani (LB)-Medium (10 g/L tryptone, 5 g/L yeast extract, 5 g/L NaCl, pH 7.4, 100 μg/mL Amp) at 37 °C and 160 rpm. The overnight culture was diluted 1:100 into 200 mL LB (

• In conclusion as illustrated in Fig

  2020-10-09

  

  In conclusion, as illustrated in Fig. 5G, in response to MNNG-induced DNA damage, PARP-1 appears to have dual roles in determining the cell fate in response to MNNG: PARP-1 activation is the cause of non-apoptotic cell death via ATP depletion and PARP-1 activation is able to elicit a self-protective

• We neither observed changes in midazolam eCLmet indicative

  2020-10-08

  

  We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c

• Phylogenetically three related CXC chemokines are classified

  2020-10-08

  

  Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e

• Apart from its high affinity

  2020-10-08

  

  Apart from its high affinity, the selection of GW2580 as Valsartan lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensiv

• N methyl d aspartate NMDA receptor antagonists such as MK

  2020-10-08

  

  N-methyl-d-aspartate (NMDA) receptor antagonists, such as MK-801 and phencyclidine, induce cognitive dysfunction in both mice and humans [18]. In addition, antipsychotic drugs ameliorate MK-801-induced cognitive dysfunction; therefore, the acute application of MK-801 can be used as an animal model o

• histone demethylase br Material and methods br Results Diagr

  2020-10-08

  

  Material and methods Results Diagrammatic representations showing the bilateral injection sites in the BNST of all animals used in the present study are presented in Fig. 1. Discussion The present results provide the first evidence that both CRF1 and CRF2 receptors in the BSNT are involved

• In the preclinical evaluation of CRF receptor antagonists

  2020-10-08

  

  In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe

• br Limitations of the study br Possible conflicts of interes

  2020-10-08

  

  Limitations of the study Possible conflicts of interest Dr. Fayemiwo or SAF has received full financial support from Europe Gilead Sciences Ltd. for his M.Sc. degree programme in Medical Mycology and has been paid for talks on behalf of AstraZeneca and GSK. Caroline Moore or CBM has received

• TMC120 Two additional hydrogen bonds are formed by the subst

  2020-10-08

  

  Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th

• Since the aggregation of neurotoxic forms of A plays a

  2020-10-08

  

  Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit

• br Acknowledgments br Introduction Cell cycle arrest or dela

  2020-10-08

  

  Acknowledgments Introduction Cell cycle arrest or delay may occur at 3 major checkpoints, i.e. G1/S, intra-S and G2/M. p53 has a central role in controlling the G1/S checkpoint, and its loss or deactivation, occurring in the majority of cancers, forces cancer cells to rely on the S and G2/M ch

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