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br Conflicts of interest br Introduction G
2021-01-25

Conflicts of interest Introduction G protein-coupled receptors (GPCRs), form the largest human membrane protein family, with 800 members overall. Many druggable targets for treatment of common diseases involve GPCRs that mediate therapeutic effects of 34% of all marketed drugs (Hauser, Attwood
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Classical DHFR inhibitors such as methotrexate
2021-01-23

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 Ivabradine HCl residues as well as hydropho
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The all NTP pyrophosphatase and NUDIX families maintain the
2021-01-23

The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes i
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In a study on the time
2021-01-23

In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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Table shows the comparison results of error
2021-01-23

Table 2 shows the comparison results of error detection rate of each software-based CFC technique. Each version of benchmark is injected 10000 errors. Even though the injected errors are randomized in spite of their classifications, the large number of injected errors guarantees that all types of CF
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It should also be noted
2021-01-23

It should also be noted that remarkable individual differences in extinguished fear bradycardia (i.e., CS+E vs. CS−E) during initial Day 2 recall test were observed, particularly within Met carriers. Exploratory analyses revealed that these individual differences were partly driven by the level of r
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In silico modelling studies might aid our understanding
2021-01-23

In silico modelling studies might aid our understanding of the functionality and potential biological activity of food and, in the long-term they might underpin the development of personalised diets to reduce health risks and help us to better understand pharmaceutical/food interactions. Acknowle
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After activation AKT phosphorylates target proteins involved
2021-01-23

After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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calculate dilution Introduction The term myeloproliferative
2021-01-22

Introduction The term “myeloproliferative disorders” was first proposed by William Dameshek in 1951. With the discovery of the Philadelphia chromosome, myeloproliferative disorders were classified into two groups: BCR-ABL positive chronic myeloid leukemia (CML) and BCR-ABL negative chronic myelopro
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For in vitro expression analysis of CXCL
2021-01-22

For in vitro expression analysis of CXCL8 and CXCRs by stimulated leucocytes, peripheral blood leucocytes (PBLs) were isolated using Percoll density gradient centrifugation as described earlier . Cell suspensions were adjusted to 5×10/ml. Four milliliters of tissue culture medium were plated per we
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It is of interest to point out that curcumin in
2021-01-22

It is of interest to point out that curcumin in this study reduced body weight gain; the underlying mechanism may be due to a decrease in general CHIR-124 of fat, which was associated with a significantly reduced NPC1L1 expression in small intestine. Labonte et al revealed that NPC1L1 deficiency or
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Molecular docking study of compound was performed using the
2021-01-22

Molecular docking study of Pefloxacin was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-h
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PKA signalling in the nucleus was
2021-01-22

PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the equol to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been identified in the nucleus and functio
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Whichever interactions are formed between the DS domains and
2021-01-22

Whichever interactions are formed between the DS domains and the collagen ligand, they are expected to lead to structural changes within the DDR dimer that are propagated across the cell membrane to result in DDR autophosphorylation (Noordeen et al., 2006). Tight coupling of the extracellular confor
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br Materials and Methods br Acknowledgements
2021-01-22

Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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