• In the present work we have investigated

  2021-08-05

  

  In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t

• The results described in the

  2021-08-05

  

  The results described in the present study confirm key restrictions on reaction conditions which must considered to maximize reactor productivity. Increased viscosity should be avoided for the amination of ketones by L-AmDH, as a 4-fold increase in viscosity can lower the reaction rate by as much as

• Next we evaluated the therapeutic potential

  2021-08-04

  

  Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone

• LY500307 Although the phase I clinical trial of LMB was unsu

  2021-08-04

  

  Although the phase I clinical trial of LMB was unsuccessful, the detailed review of this trial only mentions some malaise and anorexia as side effects, which are common for most effective chemotherapeutic drugs. These side effects may diminish if lower doses are administered. In view of the novel CR

• LPS is the major toxic component

  2021-08-04

  

  LPS is the major toxic component of the outer membrane of gram-negative bacteria and high dose of LPS challenge in animal can induce a rapid systemic inflammatory response which resembles septic shock in clinical [15]. We demonstrated that administration of KPT330 significantly attenuated lung injur

• An ideal CHK inhibitor would be minimally cytotoxic while

  2021-08-04

  

  An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th

• Compared with qualitative analysis by Kalyankar et al

  2021-08-04

  

  Compared with qualitative analysis by Kalyankar et al. (2013), less sequences were identified in iTRAQ-labelled analysis. It is not surprising with the finding that each of the identified peptide includes the sequence in every sampling point. Glu(51)-Tyr(52) of αs2-casein was observed to have been c

• Therefore HNE is an attractive therapeutic target

  2021-08-04

  

  Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo

• Recently a method for in vivo photoactivation of cells expre

  2021-08-04

  

  Recently, a method for in vivo photoactivation of PF-03084014 expressing PA-GFP in precise microanatomical compartments was described (Victora et al., 2010), which makes it possible to optically mark Tfh cells and track them 20 hr later (Shulman et al., 2013). Unexpectedly, it was reported that Tfh

• The Inhibitor of APoptosis IAP proteins were first identifie

  2021-08-04

  

  The Inhibitor of APoptosis (IAP) proteins were first identified as gene products of baculovirus that inhibited apoptosis of infected insect Paprotrain receptor (Clem et al., 1991, Crook et al., 1993). Subsequently, the mammalian IAP family was identified (Rothe et al., 1995, Uren et al., 1996). All

• br Conclusion The results of the current study show

  2021-08-04

  

  Conclusion The results of the current study show that boldness is associated with higher gene expression of drd2a, drd2b and oprd1b in zebrafish males. The results are correlational and additional experiments are needed to clarify the causal role of these receptors in zebrafish behavior. Confl

• br Results and discussion br Conclusion A

  2021-08-04

  

  Results and discussion Conclusion A new series of 2-mercapto-quinazolin-4-one analogues is designed and synthesized to possess electron withdrawing or donating functional groups (Cl or CH3O) at position 6- or 7-, 4-methoxyphenyl function at position 3. The 2-mercapto function is used to connec

• Classical DHFR inhibitors such as methotrexate MTX bind tigh

  2021-08-04

  

  Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino AICAR phosphate residues as well as hydrop

• The only in vivo evidence for a

  2021-08-03

  

  The only in vivo evidence for a role of DDR2 in fibrotic disease showed that DDR2 knockout mice exhibited exaggerated severity of chronic hepatic fibrosis. Although a previous in vitro study has demonstrated that DDR2 promotes lung fibroblast proliferation and migration, till now it remains unclear

• The first transcription factor TF known to

  2021-08-03

  

  The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone ccgs of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed development and

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