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br Conclusion br Introduction br CRL E ligases
2020-07-09
Conclusion Introduction CRL4 E3 ligases in tumorigenesis Small molecule-based PROTACs PROTAC: Major biological impacts Acknowledgements The authors sincerely apologize to all those colleagues whose important work was not cited in this paper owing to space limitations. They thank th
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In light of this our finding
2020-07-09
In light of this, our finding that UBTD1 interacts with ubiquitin conjugating enzymes is intriguing. Using two different screening approaches, we have demonstrated that UBTD1 interacts with the ubiquitin conjugating E2D family proteins. Using purified recombinant proteins and gel filtration chromato
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The Lysine mutant is located in the
2020-07-09
The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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br Conformational properties of DGK br Interaction
2020-07-09
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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Collectively the results presented here provide new insights
2020-07-09
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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In recent years the use of liquid chromatography tandem
2020-07-09
In recent years, the use of liquid chromatography/tandem mass spectrometry (LC–MS/MS) has become a preferred approach to measure drugs and metabolites in biological fluids due to its very high selectivity and sensitivity [17], [18], [19], [20], [21], [22], [23], [25], [30]. The great sensitivity of
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br Summary and perspectives In recent
2020-07-08
Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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Other karyopherins besides CRM must bind
2020-07-08
Other karyopherins besides CRM1 must bind to FG-Nups in a similar fashion. However, at an atomic resolution, only the interaction of importin β with isolated FG motifs has been analyzed (Bayliss et al., 2000, Bayliss et al., 2002, Liu and Stewart, 2005). Despite similarities in the FG-binding pocket
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IOX4 The large body of structural knowledge that is currentl
2020-07-08
The large body of structural knowledge that is currently available for CRM1 has contributed to atomic level and mechanistic understanding of many steps in the CRM1 nuclear export cycle. However, structural analysis could still inform on several outstanding questions and guide future discoveries pert
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Cell swelling stimulates the release of certain
2020-07-08
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino Cell Counting Kit-8 taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-a
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Binding affinity was measured by
2020-07-08
Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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Interferon IFN induces formation of
2020-07-07
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic IMR-1 (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial growth factor (VEGF)-
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Introduction Globally lung cancer has the
2020-07-07
Introduction Globally, lung cancer has the highest morbidity and mortality rates of all types of cancer, with 1.5 million patients newly diagnosed annually [1]. Approximately 85% of lung cancer cases are non-small cell lung cancer (NSCLC) [2]. The first-line treatment for NSCLC is surgical resectio
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In a study performed simultaneously by
2020-07-07
In a study performed simultaneously by another group, EWS-FLI-1 introduction into unsorted murine bone marrow-derived Pyridoxine HCl resulted in tumors with various phenotypes including one that is consistent with that of Ewing sarcoma [68]. The tumors expressed markers associated with Ewing sarcom
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br The synthesis of these antagonists relied heavily
2020-07-07
The synthesis of these antagonists relied heavily on Stille and Suzuki coupling reactions. The preparation of the required building blocks is presented in . Reduction of ethyl 6-bromo-2-pyridinecarboxylate with diisobutylaluminum hydride in tetrahydrofuran followed by treatment with triisopropylsi
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