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WAY-100635 maleate salt synthesis When six chemical inhibito
2020-02-20
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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br Introduction In mammals there are ten known
2020-02-20
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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br Summary and perspectives In recent decades enormous advan
2020-02-20
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
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As the COMT enzyme is primarily related to
2020-02-19
As the COMT enzyme is primarily related to prefrontal dopamine degradation (e.g., Yavich et al., 2007), the present study supports the notion that prefrontal dopamine modulates retention of fear extinction rather than within-session extinction (Abraham et al., 2014). Consistent with other studies we
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In summary A is a potent
2020-02-19
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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All tested antibodies exhibited positive immunoreactivity in
2020-02-19
All tested 6780 exhibited positive immunoreactivity in NSCLC tumors, with N’-epitope being the less expressed (both as overall positivity and number of positive cases, or intensity combined with number of positive cells, as provided by H-Score. This result is in accordance with previous studies [18
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br Introduction The cervix is a
2020-02-19
Introduction The herpes simplex virus infection is a poorly studied component of the mare’s reproductive tract. It has anatomical and biological defense mechanisms involved in the delicate balance between immunological tolerance, sperm transport and biological defense. Anatomically, the cervix i
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We report our experience using conventional cytogenetic anal
2020-02-19
We report our experience using conventional cytogenetic analysis, FISH using EWSR1 break-apart probes, RT-PCR, and Sanger sequencing to detect characteristic translocations in a total of 32 patients with ES diagnosed at Texas Children\'s Hospital over a 5-year interval. Materials and methods R
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ERRGO mice exhibited increased oxygen consumption decreased
2020-02-19
ERRGO mice exhibited increased oxygen consumption, decreased RER, high running endurance, and resistance to diet-induced weight gain. These changes are physiological hallmarks of increased aerobic capacity in mice and are a direct consequence of engineering highly oxidative and vascularized muscle b
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Also our data from this study indicate
2020-02-19
Also, our data from this study indicate that gestational GC exposure altered hematological and hemorheological parameters, however reports exist that altered blood rheological markers are associated with atherosclerosis and CVD (Tzoulaki et al., 2007). Also, the platelet to lymphocyte ratio (PLR) ha
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The present results are potentially relevant
2020-02-18
The present results are potentially relevant for understanding anxiety disorders and their treatment. Both COMT Val158Met (Lonsdorf and Kalisch, 2011, Montag et al., 2012) and neuroticism/anxiety (Clark et al., 1994, Mineka et al., 1998, Weinstock and Whisman, 2006) have been linked to the prevalen
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N Cyclopentylmethyl analog exhibited fold less potent recept
2020-02-18
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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Many studies have documented that enolase acts
2020-02-18
Many studies have documented that enolase acts as a plasminogen-binding protein and this interaction is involved in the tissue invasion and pathogenicity of the causative agents (Almeida et al., 2004; Avilan et al., 2000; Marcilla et al., 2007; Mundodi et al., 2008; Vanegas et al., 2007). Furthermor
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KSTDs are generally reported to be
2020-02-18
— Δ1-KSTDs are generally reported to be intracellular enzymes, either soluble or bound to subcellular particles. For instance, the enzymes from C. testosteroni ATCC 11996 and ATCC 17410 [50,90,99], R. equi [29], and N. simplex ATCC 6946 [52] were particulate-bound. On the other hand, the Δ1-KSTDs f
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Although the crystal structures of Atg
2020-02-18
Although the crystal structures of Atg4C and Atg4D are not available, their three dimensional structures can be acquired by homology modeling, using the structure of Atg4B as a template (Zhang, Li, Ouyang, Liu, & Cheng, 2016). In that model, the catalytic triad is conserved (Cys110/Asp345/His347 for
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