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While SCF E ligase activity
2020-12-10

While SCF E3 ligase activity was reconstituted with recombinant proteins two decades ago, the ability to probe APC/C was limited until recently because of its behemoth size. Human APC/C is a 1.2-MDa assembly comprised of 19 core subunits (one each of nine different APC subunits, and two each of five
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The Inhibitor of APoptosis IAP proteins were
2020-12-10

The Inhibitor of APoptosis (IAP) proteins were first identified as gene products of baculovirus that inhibited apoptosis of infected insect LY 235959 (Clem et al., 1991, Crook et al., 1993). Subsequently, the mammalian IAP family was identified (Rothe et al., 1995, Uren et al., 1996). All members o
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br Results and Discussion br Experimental Procedures
2020-12-10

Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac
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The roles of ginsenoside in E and S
2020-12-10

The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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br Introduction br Structure of the Ku heterodimer
2020-12-10

Introduction Structure of the Ku heterodimer associated to DNA The atomic structure of the Ku heterodimer, alone and bound to a small DNA fragment, was recently determined (Walker et al., 2001) and has significantly improved our understanding of DNA recognition by DNA-PK holoenzyme (Fig. 3). B
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br Acknowledgements We thank Dr Tai Yuan
2020-12-10

Acknowledgements We thank Dr. Tai-Yuan Yu and Miss Chun-Ping Chang for helping with the drug/DNA sequence specificity study. We also thank the Chemical Synthesis Core and the Pathology Core Laboratory of IBMS for synthesizing SL-1 and for performing the pathology analysis, respectively, and the T
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In conclusion we have discovered two new derivatives and tha
2020-12-10

In conclusion, we have discovered two new derivatives ( and ) that are potent inhibitors of DHODH. H and C NMR spectroscopic data revealed that these compounds undergo ready isomerisation at room temperature in -DMSO, but the docking studies indicate that there is neither conformation nor configurat
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Our data show a site specific interaction of DDR with
2020-12-10

Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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br Results br Discussion br Experimental Procedures br Ackno
2020-12-10

Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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Since its inception ADEPT approach
2020-12-10

Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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MS023 mg This study demonstrates that GUL affects multiple p
2020-12-09

This study demonstrates that GUL-1 affects multiple pathways/processes. As GUL-1 is likely to function as an RNA-binding protein, it is conceivable that the mRNAs involved are bound to GUL-1 as part of the regulatory function of the protein. In fact, in S. cerevisiae Ssd1 was shown to bind multiple
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Synthetic peptides have proven highly valuable in
2020-12-09

Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of
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The recombinant Scl collagen system has
2020-12-09

The recombinant Scl2 collagen system has shown capability as a biomaterial as well because of its adaptability and scalability. Scl2 was functionalized to crosslink into a hydrogel without disrupting its triple helix [130]. The Scl2–hydrogel crosslinking also did not disrupt cell adhesion and integr
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Introduction The physiological significance of hypoxia is
2020-12-09

Introduction The physiological significance of hypoxia is undisputed, although largely over looked in the cancer therapeutics field focused on DNA-damage induced by ionizing radiation or drug treatment. Regions of hypoxia occur during a range of diverse biological situations including embryogenesis
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br Introduction Estrogens play an important role
2020-12-09

Introduction Estrogens play an important role in the mu receptor (Arevalo et al., 2015). During several decades, estrogen withdrawal in women has been associated with cognitive impairment, increased Alzheimer's disease (AD) risk (Pike, 2017) and with psychiatric disorders such as schizophrenia (
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