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This structure guided the variation of the compounds aiming
2020-05-18

This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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calculate the molarity of a solution The Eph ephrin signalin
2020-05-16

The Eph–ephrin signaling system has the ability to elicit bidirectional signaling, classical forward signaling by both Eph receptor via its intrinsic tyrosine kinase activity and reverse signaling by the transmembrane ephrin ligand via its cytoplasmic domain [38], [39]. Thus when EphB4 binds with ep
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During the entire life of individual articular chondrocyte a
2020-05-16

During the entire life of individual, articular chondrocyte as well as subchondral bone receives acute or chronic stress. Joints homeostasis is maintained by biomechanical stress, as rapid loss of proteoglycan in joints occurs due to immobilization or disuse. These osteophytes are fibrocartilage cap
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br Conformational properties of DGK br Interaction of DGK
2020-05-16

Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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Apart from its high affinity
2020-05-15

Apart from its high affinity, the selection of GW2580 as difluprednate lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehe
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A previous study reported that it
2020-05-15

A previous study reported that it is unlikely that silkworm mounts a general type of immune response to all viruses (Liu et al., 2015). It is not clear whether there is a common pattern of host regulation for silkworm viruses. Spry is a general inhibitor of receptor tyrosine kinases (RTKs), which is
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Besides chemopreventive effects against oxidative DNA
2020-05-15

Besides chemopreventive effects against oxidative DNA damage we evaluated the protective effects of the three Hypericum sp. and isolated compounds against alkylating DNA damage induced by MMS in HT29 cells. Human exposure to alkylating agents, from different sources, occurs in a continuous way and i
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AZD 3965 receptor With the recent expanse of technology to e
2020-05-15

With the recent expanse of technology to evaluate synthetic lethality, new combinations with DHODH inhibitors may be uncovered (O\'Neil, Bailey, & Hieter, 2017). Many oncogenic backgrounds share synthetic lethality with DHODH. Cells with mutant PTEN have increased glutamine metabolism and are sensit
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The possibility that a carboxyl group attached to the or
2020-05-15

The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a ‘
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CPG a metalloenzyme derived from sp was
2020-05-15

CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic beta lactamase inhibitor prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by
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GNE-7915 Whether a school is private or public may also
2020-05-15

Whether a school is private or public may also be an indicator of its quality. In general, private schools have smaller class sizes which may provide a better learning environment. Lindquist and Smith (2013) state that smaller class sizes provide more opportunities for students to interact with prof
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what does the cytoskeleton do br Localization of D receptors
2020-05-14

Localization of D2 receptors in striatum One characteristic of D2Rs that has complicated their study is their expression in multiple neuronal populations within striatum, both pre- and postsynaptically (Beaulieu and Gainetdinov, 2011). In addition to spiny projection neurons (SPNs), which are the
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Our previous studies have demonstrated that the
2020-05-14

Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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br Acknowledgments Denise Fernandes acknowledges a postdoc
2020-05-14

Acknowledgments Denise Fernandes acknowledges a postdoc fellowship (SFRH/BPD/34289/2006) from the Portuguese Fundação para a Ciência e Tecnologia (FCT) of the Ministry of Science and Technology of Portugal. This work was supported by the Spanish National Plan for Research (Project Ref. CGL2011-24
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br Materials and methods br Results
2020-05-14

Materials and methods Results To investigate the effect of 17βE on cell proliferation in the human renal tubular epithelia, BrdU uptake was measured in HRTEC primary and 3D-HRTEC cultures, allowing determination of the DNA replication rate. Representative microphotographs show BrdU uptake in H
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