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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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br Substoichiometric substrate modification E ligases
2021-01-22

Substoichiometric substrate modification E3 ligases catalyze the rapid transfer of the SUMOD from the E2 enzyme to the substrate. By definition, enzymes are recycled in the reaction, allowing multiple rounds of substrate modification by a single enzyme. Thus, enzymes function at substoichiometric
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Proof of concept studies with disulfiram suggest the potenti
2021-01-22

Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and
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Our study showed that parental morphine exposure in the
2021-01-22

Our study showed that parental morphine exposure in the adulthood is associated with an increased tendency toward morphine consumption in F1 but not F2 male offspring. Thus, it seems that trans-generational effects of parental morphine consumption disappear in the second generation. In support of ou
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Having generated synthetic cytokines and synthetic cytokine
2021-01-21

Having generated synthetic cytokines and synthetic cytokine receptors, the logical next step has been to design fully synthetic cytokine/cytokine receptor systems, modifying either cytokine/cytokine receptor binding interfaces or cytokine-unrelated combinations of substances and their binding domain
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e 64 In conclusion our work led to the
2021-01-21

In conclusion, our work led to the characterization of some signalling events of the CysLT1 receptor variants, at several levels, and showed that a punctual serine mutation could alter the response of receptors to cysLTs. Although atopy is a complex phenotype implicating different cell types, mediat
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2021-01-21

Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase MK2206 synthesis [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour a
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Ligand binding RTK activation induces the endocytic internal
2021-01-21

Ligand binding (RTK activation) induces the endocytic internalization of RTKs, and this has been demonstrated for CSF-1R [15], [16], [17]. Endocytosed RTKs are targeted to the lysosome, which we and others have established to be dependent on ubiquitination via CBL-family and recognition by ESCRT com
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Nile tilapia Oreochromis niloticus is an important species f
2021-01-21

Nile tilapia (Oreochromis niloticus) is an important species farmed worldwide (Doan et al., 2018). Lipid-rich diets are commonly used in Nile tilapia aquaculture to reduce feed cost, but impair lipid homeostasis (Huang et al., 2016). Therefore, it is important to determine whether forskolin can sti
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Furthermore positioning the naphthalene nucleus in d within
2021-01-21

Furthermore, positioning the naphthalene nucleus in 3d within the main active site and forming one hydrogen bond with Tyr385 in addition to many hydrophobic interactions with Val349, Leu352, Gly526, Ala527 and Leu531 residues, correlates well with the position and hydrophobic interactions of the tri
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Due to the results of the experiment we decided
2021-01-21

Due to the results of the experiment we decided to deploy our cloud service infrastructure with two platform-independent servers instead of one or three. This decision was based on two factors: (a) the use of more than one server is useful to avoid a bottleneck in the system, and (b) using more than
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WAY-262611 australia br Funding This work was partly support
2021-01-21

Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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