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The differences between ground and transition
2019-10-23
The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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DSBs can be repaired by two major
2019-10-23
DSBs can be repaired by two major pathways: canonical non-homologous end-joining (c-NHEJ) and homologous recombination (HR) (Chapman et al., 2012). c-NHEJ comprises two sub-pathways, a resection-independent process and a resection-dependent process, and can rejoin break ends with little or no sequen
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br Introduction Epidermal growth factor receptor EGFR activa
2019-10-22
Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe
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br EBI structure and expression The gene encoding
2019-10-22
EBI2 structure and expression The gene encoding EBI2 was originally identified together with EBI1 (CCR7) as the most highly upregulated gene in Epstein–Barr virus-infected Burkitt\'s lymphoma cells [18]. EBI2 belongs to the rhodopsin-like subfamily of seven transmembrane GPCRs [19]. Although it
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Oligomycin Complex Elevation of plasma glucocorticoids as we
2019-10-22
Elevation of plasma glucocorticoids as well as a sympathetic activation are highly adaptive mechanisms allowing the individual to cope in various situations [39]. Novelty-induced increase in locomotor activity, characterizing the bold fish herein, accompanied by elevated glucocorticoids is a well-es
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Industrial fermentation aims to produce valuable products fr
2019-10-22
Industrial fermentation aims to produce valuable products from cheap feedstocks by utilizing diverse microbial functions through aerobic or anaerobic fermentation [[8], [9], [10]]. During anaerobic fermentation, the reducing power is mostly directed to product synthesis rather than being oxidized, r
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br Additional CDKs with a role in cancer br
2019-10-22
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 ‘in
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Compounds were screened for their activity against the
2019-10-22
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Notably HSP expression is under control of the tetrameric fo
2019-10-22
Notably, HSP27 expression is under control of the tetrameric form of CK2 holoenzyme, as knockout or knockdown of the β regulatory subunit alone reproduces the same effects of targeting the α/α′ catalytic subunits. This observation discloses the possibility to use more specific drugs that affects onl
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In the particular case of metals several authors
2019-10-22
In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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During the past decades HT had
2019-10-22
During the past decades HT had been widely prescribed with the expectation of both osteoporosis and cardiovascular disease prevention. The results of the Women\'s Health Initiative (WHI) trial, however, indicated that long-term HT use is associated with a small but significant increase of cardiovasc
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Targeting the MAPK pathway has attracted significant interes
2019-10-22
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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Historically covalent drugs have had great success e
2019-10-22
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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IC261 australia Acknowledgments br Introduction Diabetes mel
2019-10-22
Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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br Acknowledgment This work was supported by the Estonian
2019-10-22
Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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