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In some of our studies we
2019-10-15
In some of our studies we examined the occurrence of ERβ and SHBG and a possible colocalization between them. Fig. 5 shows that there is no big difference in the occurence of ERβ after short time (A) as well as long time (B) treatment with E2. We can find the receptor at the cell membrane as well as
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Across the scaffold the platform anchors the N terminus of
2019-10-15
Across the scaffold, the platform anchors the N terminus of the elongated cullin structure of APC2 [21]. This connects to the flexible cullin–RING catalytic core consisting of the C-terminal region of APC2 and the associated APC11 11, 12, 21. The flexibility and positions of the catalytic core are c
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br Results br Discussion The
2019-10-15
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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br Fragment based drug discovery FBDD is a
2019-10-15
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical bombesin receptor space with libraries which are smaller in size, producing drug leads with high ligand-binding efficien
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In summary synthetic routes with moderate to high yields
2019-10-15
In summary, synthetic routes with moderate to high yields have been developed to produce difluoro-dioxolo-benzoimidazol-benzamides including reference standards and , and -desmethylated precursors and , and carbon-11-labeled difluoro-dioxolo-benzoimidazol-benzamides target tracers [C] and [C]. The r
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Here two labs that helped
2019-10-15
Here, two labs that helped characterize these two pathways have worked together to further test whether these apparently parallel pathways from β-AR to CaMKII-RyR might be related in series. Much of the work leading to the Epac pathway involved measurement of Ca sparks as an index of SR Ca leak, oft
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Endothelin appears to have direct effects
2019-10-15
Endothelin 1 appears to have direct effects on neoplastic MDL 800 by inducing cellular proliferation, angiogenesis, migration, invasion, and inhibition of apoptosis [10]. Endothelin 1 mediates mitogenic effects in some epithelial tumors such as colorectal, ovarian, and prostate cancers [11], [12],
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br Materials and methods br Results br
2019-10-15
Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th
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Although in vitro and in vivo immunosuppressive effects
2019-10-14
Although, in vitro and in vivo immunosuppressive effects of female steroids have been described in fish (Yamaguchi et al., 2001, Law et al., 2001), their mode of action was not evaluated in detail. Consequently, it is of considerable interest to investigate the intracellular pathways that regulate t
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DCPIB br The modulation of ER from
2019-10-14
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective DCPIB receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, despite lac
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br Halogenases Enzymatic C H activation leading to
2019-10-14
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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Batimastat mass The synthesis of compounds a and
2019-10-14
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of Batimastat mass 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b
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In essential hypertensive patients it is known that the
2019-10-14
In essential hypertensive patients, it is known that the CB is enlarged (Habeck, 1986). In addition to morphological changes in the CB, hyperventilation was reported in essential hypertensive patients at resting conditions (Trzebski et al., 1982). Furthermore, CB is innervated by postganglionic symp
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The p controls transcription of several
2019-10-14
The p53 controls transcription of several genes that affect the release of cytochrome c in the mitochondrial apoptotic pathway [44]. In addition, p53 can induce a transcription-independent apoptosis through a direct interaction with the Bcl-2 family proteins [45]. However, the role of mitochondrial
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Almost all previously published haplotype association studie
2019-10-14
Almost all previously published haplotype association studies have demonstrated the importance of haplotype reconstruction because the combinations of SNPs exert synergistic effects on protein function. Even synonymous polymorphisms within haplotypes can have functional consequences that are drastic
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