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Estrogens Definition and history The term estrogens refers
2021-02-19
Estrogens: Definition and history The term “estrogens” refers to a group of female hormones, including estrone, estradiol, estriol, and estretrol (Fig. 1). Chemically, estrogens belong to the family of organic compounds known as steroids. As such, their core structure is composed of 17 carbon-carbo
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Grapiprant is a selective antagonist for prostaglandin E PGE
2021-02-19
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Following DEX exposure the levels of CYP A protein and
2021-02-18
Following DEX exposure, the levels of CYP1A1 protein and activity remained unchanged, as seen in our previous in vitro study (Burkina et al., 2013). Dasmahapatra and Lee (1993) reported that 3.9μgL−1 DEX, similar to our highest tested concentration, did not change CYP1A1 protein content. An increase
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In this study we have explored a functional role of
2021-02-18
In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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Next the BE obtained for the different
2021-02-16
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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br Introduction The discoidin domain
2021-02-16
Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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Since we found that the pharmacokinetic properties of
2021-02-16
Since we found that the pharmacokinetic properties of KPT-185 were unsuitable when given subcutaneously or orally, it is not a candidate for in vivo therapy for NHL. However, the pharmacokinetic properties of KPT-276, a CRM1-inhibiting SINE structurally related to and with functional activities simi
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Dextran sulfate sodium salt br Functional significance Defec
2021-02-15
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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Increasing age among middle aged subjects years
2021-02-15
Increasing age among middle-aged subjects (30–59years old) was associated with higher levels of cholesterol synthesis markers (although without statistical significance) and also of cholesterol AS 602801 synthesis markers (with statistical significance for campesterol and sitosterol); this finding i
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Other membrane currents are affected as
2021-02-15
Other membrane currents are affected as well. Some studies have provided evidence that sulfonylureas, in addition to blocking KATP channels, also inhibit chloride and calcium channels. GLYB has been shown to almost inhibit the current generated by Na+–K+ pumps in a concentration-dependent manner (wi
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BMX-IN-1 br Materials and methods br Data
2021-02-15
Materials and methods Data and statistical analysis The results were expressed as mean ± SEM. One-way analysis of variance (ANOVA), followed by Bonferroni's post-test or unpaired Student's t-test were used to determine significant differences between groups. The program used for statistical an
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The nitrophenols b d were prepared
2021-02-15
The nitrophenols 34b–d were prepared as described in Scheme 3b. Nitration of phenols 39b–d with 1equiv of sodium nitrate in the presence of hydrochloric M344 gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below. Nitration of 39b–d
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br RING dimerization RING type domains are found in many
2021-02-12
RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain Cinacalcet HCl (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7
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br Materials and methods br
2021-02-12
Materials and methods Results Discussion Although autophagy is known to be implicated in the therapeutic effect of DNA alkylating agents such as MNNG [28], [29], [30], the molecular mechanisms underlying autophagy induced by MNNG remain largely elusive. In this study, we present evidence sh
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br Materials and methods br Results The i v
2021-02-11
Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration ha
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