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External factors such as protein partners can also activate
2020-06-02
External factors, such as protein partners, can also activate DUBs by either reinforcing the stimulatory effects of intramolecular factors or by other means. The intramolecular activation of the USP7 CD by its HUBL domain is allosterically potentiated by external factor GMP synthase (GMPS), which co
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Homologous recombination HR has important roles in
2020-06-02
Homologous recombination (HR) has important roles in the repair of stalled or collapsed DNA replication forks, as well as of DNA double-strand breaks. Among the factors required for HR in human UK-5099 are RAD51, BRCA1, and BRCA2 (Davies et al., 2001, Sung and Klein, 2006, Xia et al., 2001). BRCA1
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Norfloxacin hydrochloride Everolimus treatment showed an inc
2020-06-02
Everolimus treatment showed an increase in the number of plaques and a reduction in plaque size, depending on concentration and treatment time (Fig. 1, Fig. 2). Everolimus-pretreated Norfloxacin hydrochloride adsorbed less virus with more plaque formation in the initial phase of infection (Fig. 3).
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As an endogenous negative modulator CRBN inhibits
2020-06-01
As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si
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The cysteinyl leukotrienes cysLTs LTC LTD
2020-06-01
The cysteinyl leukotrienes (cysLTs) LTC, LTD, and LTE are increased in the airways of asthmatic subjects, with the ability to induce bronchoconstriction, vascular permeability, and mucus secretion., , , , CysLTs are well established as mediators of allergic rhinitis and asthma on the basis of the e
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AMD-070 hydrochloride br Materials and methods br Results an
2020-06-01
Materials and methods Results and discussion Conclusions Conflict of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (31302162, 31171762), National High Technology Research and Development Program of China (863 Program,
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br Materials and methods br Results and
2020-06-01
Materials and methods Results and discussion Conclusions Conflict of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (31302162, 31171762), National High Technology Research and Development Program of China (863 Program,
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Cx platin could improve the level of cellular uptake and
2020-06-01
Cx-platin could improve the level of cellular uptake and DNA platination, hence triggering distinct DNA damage repair pathways. The data (Fig. 3B, C and D) demonstrated that Cx-platin could increase the foci number of γH2AX in cancer cells, preventing the efficient DSBs repair. This gives a good exp
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In order to validate the ATP
2020-06-01
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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br Introduction Cell transplantation therapies using embryon
2020-06-01
Introduction Cell transplantation therapies using embryonic stem cell (ESC) and induced pluripotent stem cell (iPSC)-derived retinal tissue (ESC/iPSC retina) or Poziotinib have emerged as therapeutic options for retinal degeneration following recent breakthroughs. A number of groups have shown t
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br Methods br Results br
2020-05-30
Methods Results Discussion On the other hand, surgical patients have to some extent stress during pre- and/or post-operative period. It is well known that CRF/CRF1 receptor is involved in the activation of HPA during acute and chronic stress (Papadimitriou and Priftis, 2009, Zelena et al.,
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In S cerevisiae Mek a paralog of the checkpoint
2020-05-29
In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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CYP contributes to the metabolism of
2020-05-29
CYP450 contributes to the metabolism of more than 90% of currently available drugs (Shapiro and Shear, 2002). Currently, CYP1A is the most studied xenobiotic-metabolizing isoform in fish and is often used as a biomarker for early effects of pollutants in aquatic organisms (Havelkova et al., 2007). T
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Bcl functions as a transcription repressor via
2020-05-29
Bcl6 functions as a transcription repressor via its N-terminal BTB domain and middle “second repression,” or “RD2” domain (Chang et al., 1996, Seyfert et al., 1996). A loss of function of the BCL6 BTB domain markedly impairs survival and proliferation of mature GC compound libraries for drug discove
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br Conclusion New series of thiazolo d pyridazine and
2020-05-29
Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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