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The phenolic hydroxyl group of ezetimibe tolerated various
2021-05-20

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 Experimental Procedures br Author Contributions M M
2021-05-20

Experimental Procedures Author Contributions M.M. and M.T. designed and supervised the study. S.I. conducted the analysis on NOG-rd mice. H.-Y.T., M.F., and T.M. conducted and analyzed MEA. S.I., H.-Y.T., and M.M. performed 3D image analysis. N.K., T.K., M.G., and R.T. planned and established
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Binding affinity was measured by a scintillation proximity b
2021-05-20

Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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pterostilbene receptor As a transcription factor HOXA regula
2021-05-20

As a transcription factor, HOXA9 regulates multiple target genes related to cell growth, including BRCA1 [34], BCL-2 [35], c-MYB [36], IGF1 [37], PIM1 [38] and so on. In addition, HOXA9 is a member of both activating and repressive transcriptional regulatory complexes, along with cofactor and collab
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br Lymphoplasmacytic lymphoma Waldenstrom macroglobulinemia
2021-05-20

Lymphoplasmacytic lymphoma/Waldenstrom macroglobulinemia Lymphoplasmacytic lymphoma (LPL) and its subgroup Waldenstrom macroglobulinemia (WM) are rare and indolent lymphomas that arise from fully differentiated B cells. The only family of GPCRs that has been well studied in LPL/WM is the chemokin
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In a study carried out
2021-05-20

In a study carried out by Aunis et al. the properties of soluble DBH and membrane bound were examined [23]. The membrane bound enzyme was shown in fluvastatin sodium to the soluble form to have thermal denaturation at higher temperatures of 43.5–44°C. Similar discontinuities in the Arrhenius plots w
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br The related catalytic regions of the human DNA
2021-05-20

The related catalytic regions of the human DNA ligases contain three domains, a DNA binding domain (DBD), a nucleotidyl transferase domain (NTase) and an oligonucleotide/oligosaccharide-fold binding domain (OBD) (Ellenberger and Tomkinson, 2008). Similar to DNA ligase I, the DNA ligase III polypep
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The on target in vitro pharmacology of was
2021-05-19

The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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br Introduction The dorsal periaqueductal gray matter dPAG i
2021-05-19

Introduction The dorsal periaqueductal gray matter (dPAG) is a midbrain site markedly involved in fear/anxiety-evoked responses as well as in nociception (see, for example, Bandler and Carrive, 1988, Deakin and Graeff, 1991, Fardin et al., 1984a, Fardin et al., 1984b, Litvin et al., 2007). Chemic
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Various domains of the HSA molecule have
2021-05-19

Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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During recent years two primary types of models
2021-05-19

During recent years, two primary types of models have been applied for calculating various thermodynamic properties of amino Alisol A solutions, i.e. excess Gibbs energy (gE) models used numerously to describe the solubility of amino acid solutions, and equations of state (EOS) models appropriate t
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To estimate the nonparametric regression we use
2021-05-19

To estimate the nonparametric regression, we use a B-spline basis. Let be the space of polynomial splines of degree and denote a normalized B-spline basis with and , where is the supremum norm. For any and , we have for some coefficients . Here we allow to increase with and differ for differ
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Cx platin could improve the level of
2021-05-19

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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Cell swelling stimulates the release of
2021-05-19

Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino Triclosan taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activated t
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ClC is a member of the voltage gated chloride channel
2021-05-19

ClC-3 is a member of the voltage-gated chloride channel superfamily and has many roles in cell proliferation, apoptosis, Acknowledgments progression and so on (Dai et al., 2005). A growing number of studies showed that ClC-3 encoded a volume-regulated Cl− channel (ICl,Vol) in heart, that could cont
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