• br Iterative design approach overview An iterative design st

  2020-11-18

  

  Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti

• br Summary and perspectives In

  2020-11-18

  

  Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are

• For most enolases fluoride acts as an

  2020-11-18

  

  For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby

• The significance of the difference in

  2020-11-18

  

  The significance of the difference in the DDR2 binding specificity towards fibrillar and non-fibrillar collagens is not understood, but may imply differences in biological responses when chondrocytes bind to different collagens in the growth plate. Investigations by Labrador et al. (2001) have shown

• peptide yy Collectively the results presented here provide n

  2020-11-18

  

  Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of

• The potent estrogen EE induced a decrease

  2020-11-18

  

  The potent ON-01910 EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) who exposed male rats

• OHC is a potent regulator of LXR mediated pathways that

  2020-11-18

  

  25-OHC is a potent regulator of LXR-mediated pathways, that impact on bms-536924 lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OHC is able to st

• The synthesis of compounds a and b are outlined

  2020-11-18

  

  The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of Venlafaxine receptor 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and

• The kinase activity of DNA PKcs is essential

  2020-11-18

  

  The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], HOAt IV [62], and XLF [6

• br Common features of TdT pol

  2020-11-18

  

  Common features of TdT, pol μ and pol λ TdT, pol μ and pol λ remain in a closed conformation throughout their catalytic cycle, contrary to pol β [24•, 53, 54•]. One possible explanation for this observation is that they have traded fidelity (which requires open-to-closed transition) for a very ti

• caudatin synthesis Previous studies from our lab looked at t

  2020-11-17

  

  Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden

• G DH has gained interest because of its broad substrate

  2020-11-17

  

  G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif

• Previous studies reported that combined administration of li

  2020-11-17

  

  Previous studies reported that combined administration of licorice/GL and TWHF/TP showed reduced toxicity and equal or even potentiated therapeutic efficacy when treating arthritis (YS et al., 2006, YS et al., 2008, Zhang et al., 2007). Our findings that GL reduced exposure to TP in rats confirmed t

• br Alcohol and the amygdala br Alcohol

  2020-11-17

  

  Alcohol and the amygdala Alcohol and the CRF1 system Given the marked effects of alcohol on inhibitory neurotransmission in the amygdala and the regulation of amygdalar GABAergic activity by CRF and activity at the CRF1 receptor, the CRF system is a logical site for the actions of alcohol in t

• Due to its several industrial applications the recombinant p

  2020-11-17

  

  Due to its several industrial applications, the recombinant production of collagen and all its derivatives as gelatins has been pursued for many years in different biological systems as mammalian Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) (Toman et al., 1999), tobacco plants (Ruggiero et

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