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In the context of E ligase drug discovery
2021-02-27
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 fil
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The death associated protein kinase DAPK is
2021-02-27
The death-associated protein kinase (DAPK) is an actin-associated, calcium/calmodulin-dependent enzyme with serine/threonine kinase activity [11], [12]. DAPK is a pro-apoptotic gene and participates in various apoptotic systems, such as TNF-α- and Fas-triggered apoptosis [10], IFN-γ-induced cell dea
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VEGFR Tyrosine Kinase Inhibitor II br Conclusion br Limitati
2021-02-27
Conclusion Limitations Conflict of interest Financial disclosure The research was supported by National Institute of Mental Health and Neuro Sciences (NIMHANS)Intramural Research Grant ID NIMH/PROJ-RSM/545/2014-15. India. Acknowledgments Introduction Increased central and peripher
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br Proteases with special focus on cysteine proteases
2021-02-27
Proteases with special focus on cysteine proteases Vaccination using cysteine proteases as antigens with special emphasis on DNA-vaccines Concluding remarks In spite of the great potential of DNA vaccines, the technology has not been as revolutionary as expected in higher mammals. In fish,
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br Introduction The allergic response is
2021-02-27
Introduction The allergic response is a complex process involving the interaction of several mediators; among these, cysteinyl leukotrienes (CysLTs) represent one of the most important actors in the pathogenesis of airway allergic diseases such as allergic rhinitis and asthma [1]. Pharmacological
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br Discussion Our data demonstrate that the bicyclam
2021-02-27
Discussion Our data demonstrate that the bicyclam AMD3100 strongly interacts with CXCR-4, whereas DS and AR177, two other compounds that also interfere with virus entry into the Vinorelbine (and interfere with virus binding), do not. AMD3100 is a unique compound in that it interferes with the che
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We have previously characterized the leucine rich NESs locat
2021-02-27
We have previously characterized the leucine-rich NESs located within the zinc-binding domains of mucosal high risk HPV16 E7 (76IRTLEDLLM84) and low risk HPV11 E7 (76IRQLQDLLL84) mediating their nuclear export in a CRM1 dependent manner (Knapp et al., 2009, McKee et al., 2013). The zinc-binding doma
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In rats exposed to day of nicotine withdrawal
2021-02-27
In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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br The LSCP model and its
2021-02-27
The LSCP model and its properties In this section, we first introduce the LSCP model in Section 2.1. Some examples of the model are presented in Section 2.2 and basic properties of the model are presented in Section 2.3. Finally, Section 2.4 introduces finite dimensional approximations necessary
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GSK-923295 br Conflict of interest statement br Acknowledgem
2021-02-27
Conflict of interest statement Acknowledgement The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7/2007-2013) under grant agreement n° 278742 (Eurosarc) Introduction Pseudomyogenic hemangioendothelioma/epithelioid sarcoma-like
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vasopressin receptor antagonists br Materials and methods br
2021-02-27
Materials and methods Results and discussion Conclusions In the present study, we have shown the important role of miR-204-5p in C2C12 myoblast differentiation. Overexpression of miR-204-5p inhibited myogenic differentiation and decreased the formation of slow-twitch myofibers, whereas miR-
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In mammals ribonucleotide reductase RNR is a
2021-02-27
In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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br Materials and methods br Results br Discussion
2021-02-27
Materials and methods Results Discussion Cells in the human body, especially in the cardiovascular and musculoskeletal systems, undergo a variety of mechanical stimuli. In order to ensure human movement, the strength of stretching muscles acts on cartilage and bone, moving joints through te
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N Cyclopentylmethyl analog exhibited fold
2021-02-27
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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br Target enzyme attributes and substrate
2021-02-27
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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