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A number of in vivo studies have
2022-01-03

A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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Nuclear export of GK has been reported to be dependent
2022-01-03

Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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br Acknowledgements br Introduction This
2022-01-03

Acknowledgements Introduction This article, similar to those before [1,2], presents a selection of nails for those red blood cell physiologists with hammers. The various topics are not necessarily lost for, like occupants on a carousel, they reappear periodically. Sometimes, however, some arti
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In the course of our
2022-01-03

In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric idasanutlin type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the proce
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br Experimental section br Results and discussion br Conclus
2022-01-03

Experimental section Results and discussion Conclusions To summarize, the act of conjugating a ASC ligands to a Ru(II) polypyridyl subunits resulted in a class of excellent DNA binders. A comparison of the DNA binding abilities of the free ASC ligand and the complexes, has revealed that the
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Tetrazole is one of the most commonly used bioisosteres for
2022-01-03

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Acknowledgments This study was supported by a Conquer Can
2022-01-03

Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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A new series of pyrimidones with C and C
2022-01-03

A new series of pyrimidones (14) with C-7 and C-9 modifications were furnished consisting of a hydroxypyridinone and a thiazole ring and checked against raltegravir resistant HIV mutant strains to determine their in vitro anti-HIV IN potency. Compounds 14a–14a, 14b–14b and 14c–14c appeared with 6.4
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individuals with variants in the codon
2022-01-03

13 individuals with variants in the codon 1031–1159 region had global developmental delay and apparent ID, ranging from speech delay and learning difficulties to markedly impaired basic life functions (Table 2 and Table S3). The last available occipitofrontal-circumference measurements revealed micr
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br Trifluoromethylketones This group of
2022-01-03

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Meropenem trihydrate mg in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the
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