• Soon after the discovery of ET and the cloning

  2020-04-22

  

  Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).

• Molecular imaging that provides a non invasive means

  2020-04-22

  

  Molecular imaging that provides a non-invasive means to visualize and measure a biological process of interest at the molecular and cellular level in living subjects has emerged as a promising approach for in vivo detection of enzyme activity in recent decades [6]. In melk inhibitor to anatomical i

• Since the dideoxy analogues and served as substrates for

  2020-04-22

  

  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 intr

• br Material and methods br Results br Discussion

  2020-04-22

  

  Material and methods Results Discussion Cysticerci located in host tissues are exposed to several effector mechanisms of the immune system (Flisser et al., 1986; Sciutto et al., 2000; Amit et al., 2011; Singh et al., 2013). In addition, the extensive uptake of host proteins by cysticerci ha

• In conclusion we have identified Ednra as

  2020-04-22

  

  In conclusion, we have identified Ednra as a downstream direct target of Hoxa9 and Meis1. Upregulation of Ednra has a role in the progression of Hoxa9+Meis1-induced leukemia and targeting Ednra together with other chemotherapies may have therapeutic benefits for leukemia [30]. Ednra inhibitors in th

• br Guidance of B cell localization

  2020-04-22

  

  Guidance of B cell localization by EBI2 EBI2 expression and B cell disease Although chemoattractant receptors of the GPR family play essential roles in coordinating the migration of lymphocytes for efficient responses against pathogens, their dysregulation can result in the initiation or progr

• Our results demonstrate that pt PGE in

  2020-04-22

  

  Our results demonstrate that 17-pt-PGE2 - in addition to its described effects on EP1 and EP3 receptors - also acts as an EP4 agonist and thereby enhances vascular barrier function. Materials and methods Results Discussion In this study we demonstrate that the purported EP1/EP3 receptor ag

• Enzyme selectivity of many enzymes like galactosidases

  2020-04-22

  

  Enzyme selectivity of many NNC 55-0396 like β-galactosidases, acylases, epoxyhydrolases, lipases, etc. has also been modulated by using different immobilization techniques. It can result in the selection of optimal biocatalyst for different processes. This has many advantages over strategies like ge

• Several research groups have disclosed potent and selective

  2020-04-22

  

  Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2

• Data on optimal hormone formulations

  2020-04-21

  

  Data on optimal hormone formulations, routes of administration, doses and duration of hormone use in young women with POF are lacking (Box 1). Transdermal Ampicillin Trihydrate mg administration, which avoids the first-pass hepatic circulation and the increase in inflammatory markers such as C-reac

• We next focused our design building into the ribose

  2020-04-21

  

  We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po

• Our finding that activating DDR variants are a cause of

  2020-04-21

  

  Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho

• Next we evaluated the therapeutic potential of

  2020-04-21

  

  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

• For any vector let and

  2020-04-21

  

  For any vector , let , and . For , let The information matrix for the partial likelihood at Eq. (2.2) can be expressed as It is well known that Wortmannin under certain regularity conditions such as (A)–(D) in Andersen and Gill (1982), where and denote the maximum likelihood estimator from Eq. (2.

• One step in pyrimidine biosynthesis is conversion of l dihyd

  2020-04-21

  

  One step in pyrimidine biosynthesis is conversion of l-dihydroorotate (DHO) to orotate (ORO), under action of the enzyme dihydroorotate dehydrogenase (DHODH, EC 1.3.99.11), which contains a flavine (FMN) as redox cofactor [1]. In this transformation, electrons resulting from DHO oxidation are transf

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