• br Iterative design approach overview An iterative

  2019-11-07

  

  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 pept

• Considering the divergence of multiple

  2019-11-06

  

  Considering the divergence of multiple DGAT isoforms, we examined whether MiDGAT1 and MiDGAT2s utilized different fatty acids as the substrate to synthesize TAGs. GC-MS analysis indicated that C16:0 and C18:0 were the major components of TAGs in yeast cells, and all three MiDGATs displayed the same

• Thienoguanosine Replacement of the saturated propoxy group i

  2019-11-06

  

  Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have di

• br Results br Discussion Many studies have shown that

  2019-11-06

  

  Results Discussion Many studies have shown that intrinsic properties of the E2 enzyme govern the nature of the Ub modification, including both the multiplicity of the Ub modification and the specific Harringtonine receptor type in the case of polyubiquitin chains [3], [4], [9], [14]. Whereas

• Nuclear export mediated by CRM is initiated by an

  2019-11-06

  

  Nuclear export mediated by CRM1 is initiated by an interaction between RanGTP and the HEAT9 loop of CRM1, triggering a conformational change in the NES binding site that permits NES–cargo protein binding (Dong et al., 2009, Fung and Chook, 2014). Our docking simulation results predicted that DP2392-

• br Materials and methods br Results br Discussion In this

  2019-11-06

  

  Materials and methods Results Discussion In this study, we confirmed the activation of Akt by udenafil in 3T3-L1 cells. To elucidate the underlying mechanism of udenafil, we focused on the mitochondria. Our findings demonstrated that udenafil improved mitochondrial function and expression o

• In sum although it is reasonable to assume

  2019-11-06

  

  In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different or

• HTH-01-015 mg Since the dideoxy analogues and served as

  2019-11-06

  

  Since the 1,2-dideoxy analogues, and , served as substrates for TgTCEA and TgTCEB, respectively, with the higher affinity (lower ) and lower turnover number (lower ) than their authentic substrates, PosA and PosB (such trend was more evident on analogue for TgTCEB than on analog for TgTCEA), an int

• br E mediated E discharge E ligases

  2019-11-05

  

  E3-mediated E2 discharge E3 ligases simultaneously interact with the substrate and the SUMOD charged E2 enzyme to catalyze the discharge of the thioester-bound SUMOD from the E2 to the substrate. E3 interaction with SUMOD via a SIM results in a closed conformation which is highly reactive and lea

• br Regulation of p via the ubiquitin proteasome pathway

  2019-11-05

  

  Regulation of p53 via the ubiquitin-proteasome pathway Studies into regulation of p53 via PTM processes that involve phosphorylation, acetylation, ubiquitination, SUMOylation, neddylation, and methylation are being increasingly reported [23], [24]. Phosphorylation and acetylation of p53 stimulate

• This study had some limitations

  2019-11-05

  

  This study had some limitations. First, a small number of HP patients were enrolled because of the extreme rarity of this disease, which may have caused some selection bias. Yokoseki et al., found no increase in Th2 cytokines, such as IL-4, in IHP patients (Yokoseki et al., 2014). The sensitivity of

• Cytochrome P CYP enzymes plays an

  2019-11-05

  

  Cytochrome P450 (CYP-450) enzymes plays an essential role in pharmacology of drugs and toxicology of xenobiotics. Inhibition of these enzymes may lead to increase plasma levels of a concomitantly administered drug (Lee et al., 2013). It may prolong or reduce the pharmacological effects and increase

• In contrast to PEGylated proteins which tend to have

  2019-11-05

  

  In contrast to PEGylated proteins which tend to have reduced NCT-502 mg in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applications in the field of ch

• br Diseases which have been treated with proteins linked to

  2019-11-05

  

  Diseases which have been treated with proteins linked to HSA A number of therapeutic products conjugated to HSA have now been approved for clinical use (Table 2). For example, fatty salinomycin derivatives of human insulin bound to HSA have applications in the treatment of diabetes while paclita

• ly411575 receptor In addition to PDCA we also tested

  2019-11-05

  

  In addition to 2,4-PDCA, we also tested other broad-spectrum 2OG oxygenase inhibitors as vCPH inhibitors. N-Oxalyl glycine (NOG, IC50 = 21.2 ± 2.1 µM), a close 2OG isostere, and IOX1 (IC50 = 47.2 ± 2.7 µM), which is a relatively broad-spectrum JmjC demethylase inhibitor, were not as potent in inhibi

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