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There was a good alignment profile between compound IC
2021-06-16
There was a good alignment profile between compound 26 (IC50 0.06μM) and MTX (IC50 0.08μM) explaining its activity pattern (Fig. 5a). Fig. 5b clearly indicates a different alignment profiles where carbonyl groups are not on the same side between 25 (IC50>100.0μM) and MTX which is in consistency with
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DDR expression is upregulated in the
2021-06-16
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident eg5 is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favor to this
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To extend these toxicity minimization
2021-06-16
To extend these toxicity minimization strategies to 3D tissues, a more complicated mass transfer model is necessary to account diffusion in the interstitial space, as well as transport across cell membranes. Until recently, tissue mass transport in cryobiology was modeled using classic spatially dep
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Michel et al calculated the mutual solubilities of water and
2021-06-16
Michel et al. [34] calculated the mutual solubilities of water and hydrocarbons by a cubic equation of state. They asserted that conventional mixing rules can not satisfactorily describe the hydrogen bonding compounds. Kabadi and Danner [35] applied a modified form of Soave-Redlich-Kwong equation of
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Completion of h of education was significant
2021-06-16
Completion of 150 h of education was significant in virtually all prior studies of the 150-h requirement (Allen and Woodland, 2006, Boone et al., 2006 and others). While the 150-h requirement applies to licensure, students are often permitted (as in California) to sit for the CPA exam with fewer tot
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br STAR Methods br Author Contributions br Acknowledgments
2021-06-15
STAR★Methods Author Contributions Acknowledgments The authors thank Monika Kuhn for excellent technical assistance and Dr. Antje Schäfer for valuable scientific input. H.S. was supported by the DFG (FZ 82; Graduate School of Life Sciences and SCHI 425-6/1), and A.V.S. by Northwestern Univer
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br Significance Ubl post translational modifications are pot
2021-06-15
Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig
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br Acknowledgements The study of RING
2021-06-15
Acknowledgements The study of RING-type E3s continues to grow extremely rapidly. We regret that it was possible to only cite a fraction of the outstanding primary publications in this field. This work was supported by the National Institute of General Medical Sciences grants R01 GM088055 and R01
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One of the isolated interactors against Mulan
2021-06-15
One of the isolated interactors against Mulan259–352–Ube2E3 fusion bait was found to be the GABARAP protein, a known member of the Atg8 family that includes LC3 [20]. The Atg8 family-of-proteins are major players in autophagy/mitophagy since they are part of the autophagosome [20], [21], [22]. Our s
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The quaternary structure of many of the family
2021-06-15
The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and Tylosin tartrate receptors) have been actively studied and it has been demonstrated that they can form homodimers/oligomers (Gao et al., 2009; Ng & Chow, 2015; Ng, Lee, & Chow, 2013). Harik
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Introduction Trichloroacetic acid TCA might enhance the acti
2021-06-15
Introduction Trichloroacetic Alfacalcidol (TCA) might enhance the activation of T cells and disrupt various activities of peripheral T cells [1], which is related to human immune function and reduces human immunity. Trichloroethylene (TCE) has been widely used in many manufacturing industries [2],
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Present malarial chemotherapies mainly rely on a very
2021-06-15
Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa
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In order to derive a better understanding of the
2021-06-15
In order to derive a better understanding of the results from our SAR study, we utilized Glide to model the binding of the SAR compounds with the non-active site pocket of TS-DHFR shown in C. The majority of models position the phenolic moiety of these compounds within the non-active site pocket, wh
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Compound was advanced to a chronic
2021-06-15
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, SB505124 mg 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily
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Vanoxerine In contrast to DDR the role of
2021-06-15
In Vanoxerine to DDR1, the role of oligomerization and/or clustering of DDR2 in mediating its interactions with collagen is less understood. Current data show that in DDR2, like in DDR1, (i) dimerization [7] and higher-order oligomerization of its ECD [11], [22] enhance its binding to collagen, and
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