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Classical DHFR inhibitors such as methotrexate MTX bind tigh
2021-08-27
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Deferoxamine residues as well as hydrophobi
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We have performed our MSP analyses as
2021-08-27
We have performed our MSP analyses as real-time PCR using SybrGreen (Fig. 2). The results of the beta-actin PCR vary in each sample group because the amount of DNA for bisulfite treatment was adjusted to a constant volume of serum (500μl) rather than to equal amounts of DNA. Because we expected lowe
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br P Y receptor structure br Pharmacology Several subtype se
2021-08-27
P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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In the present study it was found that
2021-08-27
In the present study, it was found that HepG2, H4IIE and LMH cells were inclined to remove S-metalaxyl and lead to decrease of ERs of metalaxyl, while L8824 cells were inclined to attenuate R-metalaxyl and resulted in an inverse shift of ER. These findings indicate the enantioselective accumulation
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van Linden et al developed a comprehensive guide
2021-08-27
van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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br Results and discussion Compounds were tested
2021-08-27
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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We next examined the effects of substituents around the carb
2021-08-27
We next examined the effects of substituents around the carboxylic Protionamide moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxylic
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The selective estrogen receptor modulators SERMs are another
2021-08-27
The selective estrogen receptor modulators (SERMs) are another type of estrogen receptor ligands. The main difference between SERMs and xenoestrogens relies on the fact that SERMs present functional duality and are able to act both as agonists and antagonists of the estrogen receptors in different t
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br Introduction Breast cancer is the most common malignant
2021-08-27
Introduction Breast cancer is the most common malignant tumor in women and the second leading cause of female death [1]. In recent years, with the improvement of early detection and the emergence of new treatment methods, the mortality rate of breast cancer has been greatly reduced. However, the
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For immobilization of enzymes natural polymers depict severa
2021-08-27
For immobilization of enzymes, natural polymers depict several outstanding features as support. These materials are inert, non-toxic, biodegradable and biocompatible. As well as, they can be treated with different functional groups easily by chemical reactions that occur under gentle conditions in a
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br Acknowledgements br Introduction Supramolecular collagen
2021-08-26
Acknowledgements Introduction Supramolecular collagen assemblies are crucial for the mechanical stability of animal bodies (Myllyharju and Kivirikko, 2004). The basic collagen structure is a triple helix of three chains containing multiple Gly-X-X' repeats; X and X' are often proline and 4-hyd
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The molecular mechanisms regulating the differentiation of T
2021-08-26
The molecular mechanisms regulating the differentiation of Th1 versus Tfh unless from IL-12-stimulated CD4+ T cells remain largely uncharacterized in humans. This topic has been extensively studied in mice (Weinmann, 2014), because IL-12 stimulation promotes mouse naive CD4+ T cells to express both
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Initially the cause of hypoglycemia was not apparent There w
2021-08-26
Initially, the cause of hypoglycemia was not apparent. There was no detectable lesion in the pancreas on plain computed tomography, and anti-insulin antibody was negative. Eight hours after hospital admission, his son discovered that the patient had accidentally taken glimepiride 3mg/day for 3 days.
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Addressing whether impaired activation of D and D
2021-08-26
Addressing whether impaired activation of D1 and D2 receptors regulates memory capacity is relevant for all human pathologies that lead to reduced activation of these Mouse Angiopoietin-2 / ANG2 / ANGPT2 Protein (His Tag) pathways, such as ageing [39], certain genetic polymorphisms [40] and neurod
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As mentioned above there are two
2021-08-26
As mentioned above, there are two major pathways for the DSB repair in mammalian cells, NHEJ and HR/HDR (homology-directed repair) [13], [51]. NHEJ is active throughout the cell cycle, predominately during the G0 and G1 phases and is considered the major pathway for the DSB repair in human cells [52
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