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There was a good alignment profile
2020-11-11
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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We aim to apply the same technology to target other
2020-11-11
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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br Introduction Natural killer NK
2020-11-11
Introduction Natural killer (NK) cells have an unique ability to directly lyse transformed, virus-infected or stressed cells without prior sensitization or major histocompatibility complex (MHC) class I restriction [1], [2]. They were initially defined and shown to be important effectors of the i
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br Additional CDKs with a role in cancer br Small
2020-11-11
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘i
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br Clinical trials of CRM
2020-11-11
Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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Nile tilapia Oreochromis niloticus is an important species f
2020-11-11
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 stim
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The crystal structure of LiCoO is presented in
2020-11-11
The crystal structure of LiCoO2 is presented in Fig. 1. We can notice that the Li and Co atoms occupy the centers of two different edge-sharing [CoO6]-octahedra, which results in formation of separate Li and Co layers. Hence, the layered structure of LiMO2 is able to intercalate lithium into transit
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Previously published data showed an
2020-11-11
Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino osmi sequence (Supplementary T
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br Effects of estrogens on
2020-11-11
Effects of estrogens on bone Estrogens play an important role in bone remodeling, as demonstrated by studies in mice in which the ER genes were deleted [21], [22]. ERβ compensates for the auda of ERα, and vice versa, but when both ERs are deleted a profound decrease in trabecular bone volume is
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br Experimental Procedures br Acknowledgments br Introductio
2020-11-10
Experimental Procedures Acknowledgments Introduction Bisphenol A (BPA), 2,2-bis (4-hydroxyphenyl) propane, is widely used to manufacture consumer products including food and beverage containers (Vandenberg et al., 2007). It can be accumulated in human body via leaching from the polymers int
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The optimization of the lead compound was initiated and the
2020-11-10
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic PKR Inhibitor moiety with other functional groups led to loss of functional activity against EP4 receptor.
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In conclusion our study has demonstrated that PGE
2020-11-10
In conclusion, our study has demonstrated that PGE2 stimulates expression of survivin in hepatocellular carcinoma cells. Although there are 4 subtypes of EP receptors, the EP1 receptor appears to be the predominant receptor that regulates PGE2-induced expression of survivin, mainly through trans-act
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During the course of enzymatic digestion protein is
2020-11-10
During the course of enzymatic digestion, protein is digested into large peptides and these large peptides are then further digested into small fragments. αs1-Casein f15–39, which contains 25 amino smoothened residues was the longest iTRAQ-labelled peptide identified in the samples digested with GE
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br Experimental Procedures br Author
2020-11-10
Experimental Procedures Author Contributions Acknowledgments We acknowledge Géraldine Le Goff and Mathieu Canales for blood sampling, Cécile Gameiro and Jean-Pierre Aubry for flow cytometry technical assistance, Giuseppe Pantaleo for support, and Britta Engelhardt, Gisella Puga-Young, Nicol
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Gabapentin The TELI results of DNA damage responses to CAA a
2020-11-10
The TELI results of DNA damage responses to CAA and SO then informed our choice of bacterial strains in subsequent experiments. We investigated E. coli cellular survival in response to CAA and SO exposure by determining the sensitivity of a number of E. coli strains, each possessing single or multip
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