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Tetrazole is one of the
2021-09-02
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Introduction The alternative splicing of pre
2021-09-02
Introduction The alternative splicing of pre-mRNA is essential for generating multiple matured mRNAs from a single gene by selectively removing introns. Neural Aloperine show many examples of regulated alternative splicing events, which produce structural changes in proteins important for the dev
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Next we studied the effects of the
2021-09-02
Next, we studied the effects of the compounds PA-Glu, PA-hSuc, and PA-hPim on the IGly of rat hippocampal neurons. As in the experiments with IGABA, IGly was affected by steroids with a pregnane skeleton, but not those with an androstane skeleton. At the same time, androstane steroids were shown to
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br Hydroxyfarnesyl diphosphate was synthesised
2021-09-02
12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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The site of paracetamol action
2021-09-02
The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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With respect to the muscle compartment only low
2021-09-02
With respect to the muscle compartment, only low protein expression of ASB9 has been detected in healthy human skeletal muscle [as reported in the Human Protein Atlas (HPA)], whereas high levels of Asb5 protein expression are detected in mammalian skeletal muscle, which appears to be important in th
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GLP signaling mediates important renal functions as suggeste
2021-09-02
GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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These data from developing brain
2021-09-02
These data from developing daunorubicin australia are in contrast to noradrenergic receptor regulation in the adult brain. In adult animals, a persistent increase in the α2-AR high affinity state is elicited as a result of DSP-4 lesion or reserpinization, as measured by [3H]clonidine binding to memb
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br Acknowledgment This work was supported by the Estonian Sc
2021-09-02
Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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Previous in vitro studies have demonstrated that DNA
2021-09-02
Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM Splitomicin (MO59K) to
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Although it is believed that CYP induction is regulated
2021-09-01
Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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A variety of fused membered
2021-09-01
A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG
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We have previously reported the characterization of A a
2021-09-01
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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br Materials and methods br Results
2021-09-01
Materials and methods Results Discussion The effect of progestogen treatment showed some tendencies affecting the body length and weight, however these data were not verifiable statistically. This observation could be explained with the relatively short exposure period and/or the relatively
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In the literature we can find two different modes of
2021-09-01
In the literature, we can find two different modes of action for estrogens: Firstly there is the commonly accepted genomic pathway. Estrogens pass the cell membrane due to their lipophilic character via diffusion and bind to estrogen receptors (ERs) in the cytoplasm. After binding a dimerization of
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