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Survival analysis has been widely
2019-09-12
Survival analysis has been widely used in medical science, economics, finance, and social science, among others. In many studies, survival data have primary outcomes or responses that are subject to censoring. The Cox model [7], [8] is the most commonly used regression model for survival data, and t
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This paper proposes an acceptance process and
2019-09-12
This paper proposes an acceptance process and evaluation criteria, specialized for the dedication of indirect COTS SW as well as direct ones. (Step 1) It first recognizes an indirect COTS SW as a target of dedication, unlike EPRI NP-5652/TR-106439. (Step 2) It then determines the safety category of
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Udenafil also has shown the ability to
2019-09-12
Udenafil also has shown the ability to significantly inhibit the decrease of vascular endothelial cell function and inhibit the decrease in endothelial cell and smooth muscle contents, thus preventing their fibrosis within the penile corpus cavernosum in diabetic or hyperlipidemic animal models when
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Akt Inhibitor IV One possible pitfall of using EPAC activato
2019-09-12
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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In studies directed toward the development of
2019-09-11
In studies directed toward the development of sequence-specific major-groove binding small Golgicide A [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode and
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This hydrophobic biphenyl tail gave good
2019-09-11
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC MK-3207 HCl was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which were
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The following is the supplementary data related
2019-09-11
The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter
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br Results br Discussion The
2019-09-11
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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Till date several predictive models have been developed by d
2019-09-11
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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An AmDH is engineered by mutating two conserved amino
2019-09-11
An AmDH is engineered by mutating two conserved amino IL-10, human recombinant protein residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions,
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Introduction Cysteinyl leukotrienes CysLTs LTC
2019-09-11
Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic CHIR-124 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3], [4] and montelukast
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More recently it was discovered that BChE hydrolyzes the
2019-09-11
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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Previous studies have documented that
2019-09-11
Previous studies have documented that SCFAs may elicit effects on lipid metabolism via de novo synthesis and transport. Acetate is not only used as an energy source, but is also constituted as a substrate for the cholesterol synthesis in the liver through acetyl-CoA, thus affecting plasma cholestero
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We have previously reported the
2019-09-11
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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We have previously reported the
2019-09-11
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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