• We have reported previously that aminoacrylate derivatives o

  2019-12-17

  

  We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD

• The different serotypes A G have unique receptors

  2019-12-16

  

  The different serotypes (A-G) have unique receptors to which they bind to produce the toxic effect on the nerve cells. (Lance, 2004, Rosetto et al., 2014). Intracellularly, the endopeptidase activity of different serotypes of BoNT target selectively a unique group of proteins, the SNARE Methylpiperi

• br Results The AR genotype frequencies are shown

  2019-12-16

  

  Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find

• br Conclusion In vivo pharmacokinetic studies

  2019-12-16

  

  Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokinet

• From the general synthetic route we

  2019-12-16

  

  From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder

• The mechanisms in the central nervous system CNS

  2019-12-16

  

  The mechanisms in the central nervous system (CNS) controlling the sympathetic tone of the experienced are associated to behavioral strategies, such as those involved in response to stress. In this regard, morphine withdrawal induces profound and severe stress reactions evidenced by enhancement of

• To the best of our knowledge this study

  2019-12-16

  

  To the best of our knowledge, this study was the first to demonstrate in vitro and in vivo that the lipolytic effect of kinsenoside results from coordination between PKA and AMPK pathways. We validated the lipolytic effect of kinsenoside in vivo and the effect of PKA activation on the modulating AMP

• We next turned our attention to the

  2019-12-16

  

  We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a

• A number of chemical strategies have been developed to desig

  2019-12-16

  

  A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai

• br Materials and methods br Results and

  2019-12-16

  

  Materials and methods Results and discussion Concluding remarks Enzymatic production of bioactive 9-cis-11-trans-conjugated linoleic icrt is part of a detoxification mechanism against linoleic acid which is a toxic and stress factor for many lactic bacteria such as Lactobacillus plantarum.

• We also found downregulation of TRIM in the

  2019-12-16

  

  We also found downregulation of TRIM32 in the hearts of dilated and hypertrophic cardiomyopathy patients in addition to TAC and phenylephrine treated mice [51]. TRIM32 and Dysbindin are known to interact in skeletal muscle, and we could confirm this interaction in cardiomyocytes as well. In cardiomy

• Dipeptidyl peptidase inhibitors DPP is

  2019-12-16

  

  Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit AGI-5198 receptor secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good effic

• Our study showed that parental morphine exposure in

  2019-12-16

  

  Our study showed that parental morphine exposure in the adulthood is associated with an increased tendency toward morphine consumption in F1 but not F2 male offspring. Thus, it seems that trans-generational effects of parental morphine consumption disappear in the second generation. In support of ou

• Herein we designed a strategy utilizing the target

  2019-12-16

  

  Herein, we designed a strategy utilizing the target-protection method to produce a signal in a system involving fluorescence CuNPs stabilized by dumbbell template DNA (DT DNA) through a locked circle consisting of two poly T loops and a poly (ATTA) stem. In the presence of MTase, DT DNA was modified

• Replacement of the saturated propoxy group in compound with

  2019-12-16

  

  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

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