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TKI discontinuation studies demonstrate that a portion of TK
2020-01-13

TKI discontinuation studies demonstrate that a portion of TKI-treated CML patients remain in remission for up to 3 years, although long-term risk assessment is still necessary (Bansal and Radich, 2016). The majority of CML patients depend on lifetime TKI treatment, and substantial efforts have been
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Furan analogs and N methylpyrrole analogs had completely
2020-01-13

Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 Koumine affinity and an increased antagonist activity, while the corresponding chemical modificat
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br Funding This work was supported
2020-01-13

Funding This work was supported by the grants from MSD, Terumo Life Science Foundation, Takeda Science Foundation, and Japan Diabetes Foundation. Disclosures Acknowledgments The authors thank C. Morimoto (Juntendo University, Tokyo, Japan) and K. Takeda (Immunology Frontier Research Center
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br Materials and methods br Results
2020-01-13

Materials and methods Results Discussion The first DGAT1 gene was described in the mouse in 1998 [28], and a few years later DGAT2 was identified from the oleaginous fungus Mortierella ramanniana[29]. Although both of them are known as the primary enzymes for de novo TAG biosynthesis, they
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We had earlier reported that collagen
2020-01-13

We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen
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Despite its significance in tumor suppression
2020-01-13

Despite its significance in tumor suppression, the molecular mechanism by which DAPK is regulated and its interplay with other tumor suppressors and oncoproteins have not been completely unraveled. Although primarily regulated by CaM binding (Cohen et al., 1997), DAPK activity can also be modulated
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br Acknowledgments br Casein kinases CK
2020-01-11

Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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SIRT has deacetylated regulation on numerous nonhistone prot
2020-01-11

SIRT1 has deacetylated regulation on numerous nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016) to play a key role in protecting against cell stress. Therefore, the role of SIRT1 in fluorine-induced oxidative stress was explored. The results reveal
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br Advent of SMEPT br
2020-01-11

Advent of SMEPT SMEPT for localized synthesis of nitric oxide Critical evaluation and outlook Examples discussed in this review present SMEPT as a methodology for localized drug synthesis – a unique opportunity for site specific therapeutic interventions using implantable biomaterials. This
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The in vitro enantioselective metabolism of pesticides has b
2020-01-11

The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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br Additional CDKs with a
2020-01-11

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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Deazaneplanocin The results of bisaryl ether
2020-01-11

The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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Although it is well established that estrogen and
2020-01-11

Although it is well established that estrogen and ESR1 mediate numerous reproductive processes, increasing evidence suggests that ESR2 also lays an integral role in reproduction. ESR2 is a mediator in folliculogenesis and may also act by stimulating ovulation and regulating luteinization (Su et al.,
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As demonstrated by Mak and colleagues ER is known
2020-01-10

As demonstrated by Mak and colleagues, ERβ is known to be a part of the NFκB-HIF-1α signaling pathway during hypoxia as well as chronic inflammation of prostate (Mak et al., 2015), therefore in the next part of the study, we evaluated whether ZEA-induced ROS production is also associated with NFκB-H
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br Materials and methods br Results and
2020-01-10

Materials and methods Results and discussion Concluding remarks Enzymatic production of bioactive 9-cis-11-trans-conjugated linoleic s equol is part of a detoxification mechanism against linoleic acid which is a toxic and stress factor for many lactic bacteria such as Lactobacillus plantar
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