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Hepatic drug metabolizing enzymes and transporters expressio
2022-05-26
Hepatic drug-metabolizing Doripenem and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes of nuclear recepto
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LbGlcK crystallized as a ligandless dimer in the asymmetric
2022-05-26
LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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br Conflict of interest statement
2022-05-26
Conflict of interest statement Acknowledgments Introduction Hedgehog (Hh) signaling controls key steps of development in most tissues and organs of invertebrates and vertebrates (Briscoe and Therond, 2013, Ingham et al., 2011, Wilson and Chuang, 2010). The unique cellular composition and mo
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Serotonin hydroxytryptamine HT is a monoamine with dual
2022-05-26
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the Erlotinib receptor as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and Co
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bcrp inhibitor Prior to proceeding to the main tests
2022-05-26
Prior to proceeding to the main tests, essential conditions were optimized. At first, we tested whether the parameters that were successful in inducing LacZ gene for the production of β-galactosidase enzymes in E. coli culture system in our previous study would be sufficient to induce LacZ gene in t
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This review is an overview on the ongoing trials
2022-05-26
This review is an overview on the ongoing trials involving anti-FGF-FGFR therapies (Wu et al., 2013). Pathway FGFR in cancer A recent study comparing more than 4800 tumor tissue samples has shown that 7.1% of all tumor types have genetic alterations in the FGF-FGFR axis. The aberrations perce
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In terms of cytotoxicity studies under two dimensional cell
2022-05-26
In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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In conclusion a novel series
2022-05-26
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen Heparin sodium had a remarkable effect on the GPR40 agonistic activ
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GS-9973 The ability to metastasize is the defining
2022-05-26
The ability to metastasize is the defining character of a cancer and the leading cause for resultant mortality. It is hypothesized that a rare subset of cancer cells, often operationally referred to as “cancer stem cells” (CSCs), are responsible for sustaining cancer metastasis and recurrence [1]. T
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br Place in Therapy In the case of minor
2022-05-26
Place in Therapy In the case of minor bleeding, the anticoagulant effects of all FXa inhibitors except betrixaban, which has a longer half-life, will diminish within 24-48 hours of discontinuation of the drug provided the patient has normal renal function. In these cases stopping the FXa inhibito
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The characterization of Da CTSL shows that it preferentially
2022-05-25
The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a phorbol 12 myristate 13 acetate phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when
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Of xenobiotic quinones thymoquinone methyl isopropyl benzoqu
2022-05-25
Of xenobiotic quinones, thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; Fig. 1) is one of the most thoroughly studied for its pharmacological properties. It is the most active component of Nigella sativa, commonly called black cumin2, 3, the essential oil of the seeds of which are used for trea
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br Acknowledgments This research was partially supported by
2022-05-25
Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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The PI K PTEN Akt mTORC GSK pathway also
2022-05-25
The PI3K/PTEN/Akt/mTORC1/GSK-3 pathway also plays key roles in metabolism, obesity, diabetes and cardiovascular diseases (, , , , ). Sometimes such clinical problems such as diabetes, obesity and metabolic disorders are interlinked with cancer. Clearly further elucidation of the roles of GSK-3 could
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Introduction Glycogen synthase kinase GSK is an enzyme playi
2022-05-25
Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and doxorubicin hydrochloride is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconso
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