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The phenolic hydroxyl group of
2019-11-15

The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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br Materials and methods br Results br Discussion Human Chk
2019-11-15

Materials and methods Results Discussion Human Chk, a member of the Csk-family, was initially cloned from two different megakaryocytic cell lines [2], [3]. Structural comparison of human Chk with human Csk shows that human Chk has the additional N-terminal unique domain [2], [3], [25]. Chk
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br Materials and methods br Results br Discussion
2019-11-15

Materials and methods Results Discussion DDR2 played a role in cell motile behavior, but the relationship between motility and collagen activation of DDR2 tyrosine kinase was unclear. Studies with smooth muscle cells from DDR1−/− mice demonstrated a defect in cell attachment to collagen and
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In humans CYP A major isoforms of CYP As
2019-11-15

In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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In recent years there has
2019-11-15

In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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br Materials and methods br Results To investigate
2019-11-15

Materials and methods Results To investigate the effect of 17βE on cell proliferation in the human renal tubular epithelia, BrdU uptake was measured in HRTEC primary and 3D-HRTEC cultures, allowing determination of the DNA replication rate. Representative microphotographs show BrdU uptake in H
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Although it is well established that estrogen and ESR
2019-11-15

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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AZD-5438 mg A French cohort study reported that micronized p
2019-11-15

A French cohort study reported that micronized progesterone or didrogesterone used with oral or percutaneous estradiol showed no increase or decrease in the risk of breast cancer compared to synthetic progestins for at least 4 years of treatment [22] and even after 8 years [23]. Although the results
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It has only recently been appreciated that antigen activated
2019-11-14

It has only recently been appreciated that antigen-activated By design undertake two additional transient migrations during the early stages of T-dependent antibody responses. In the first of these, antigen-activated B cells migrate rapidly (within 2–3h) to the outer regions of the follicle before
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br Funding This work was supported by
2019-11-14

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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Once sufficient single stranded DNA ssDNA
2019-11-14

Once sufficient single-stranded DNA (ssDNA) has been exposed at origins, synthesis of leading and lagging strands is initiated by the DNA polymerase α-primase complex (Pol α). Lagging-strand synthesis requires repeated cycles of Pol α-dependent priming and subsequent primer extension by Pol δ. Pol α
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br Introduction Coping with DNA damage is possible thanks to
2019-11-14

Introduction Coping with DNA damage is possible thanks to surveillance mechanisms (checkpoints), that detect the problem and promote its solution [1], [2], and to repair and tolerance pathways that remove the lesions or reduce the damage consequences [3], [4]. Failures in these processes have a h
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Indeed the alkyl group is not seen
2019-11-14

Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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br Results br Discussion The
2019-11-14

Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into Clofazimine by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by their inhi
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LDC1267 australia Having generated synthetic cytokines and s
2019-11-14

Having generated synthetic cytokines and synthetic cytokine receptors, the logical next step has been to design fully synthetic cytokine/cytokine receptor systems, modifying either cytokine/cytokine receptor binding interfaces or cytokine-unrelated combinations of substances and their binding domai
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