Search Results - "Imamura, Riyo"
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Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors
Published in Chemical & pharmaceutical bulletin (01-03-2022)“…MS is a powerful methodology for chemical screening to directly quantify substrates and products of enzymes, but its low throughput has been an issue…”
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2
p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming
Published in Nature communications (27-06-2016)“…p62/Sqstm1 is a multifunctional protein involved in cell survival, growth and death, that is degraded by autophagy. Amplification of the p62/Sqstm1 gene, and…”
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3
Inhibitors of the protein-protein interaction between phosphorylated p62 and Keap1 attenuate chemoresistance in a human hepatocellular carcinoma cell line
Published in Free radical research (01-12-2020)“…Resistance to anticancer agents has been an obstacle to developing therapeutics and reducing medical costs. Whereas sorafenib is used for the treatment of…”
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4
Dephospho-Coenzyme A Kinase Is an Exploitable Drug Target against Plasmodium falciparum: Identification of Selective Inhibitors by High-Throughput Screening of a Large Chemical Compound Library
Published in Antimicrobial agents and chemotherapy (15-11-2022)“…Malaria is a mosquito-borne fatal infectious disease that affects humans and is caused by parasites, primarily Plasmodium falciparum. Widespread drug…”
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5
Restoration of Cardiac Myosin Light Chain Kinase Ameliorates Systolic Dysfunction by Reducing Superrelaxed Myosin
Published in Circulation (New York, N.Y.) (20-06-2023)“…Cardiac-specific myosin light chain kinase (cMLCK), encoded by , regulates cardiac contractility through phosphorylation of ventricular myosin regulatory light…”
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6
Molecular action of larvicidal flavonoids on ecdysteroidogenic glutathione S-transferase Noppera-bo in Aedes aegypti
Published in BMC biology (17-02-2022)“…Mosquito control is a crucial global issue for protecting the human community from mosquito-borne diseases. There is an urgent need for the development of…”
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Synthesis of both enantiomers of 1,2,3,4-tetrahydroisoquinoline derivative IPPAM-1 and enantio-dependency of its positive allosteric modulation of prostacyclin receptor
Published in Bioorganic & medicinal chemistry letters (01-06-2017)“…[Display omitted] We present a practical synthesis of both enantiomers of 1,2,3,4-tetrahydroisoquinoline derivative IPPAM-1 (1), which is a positive allosteric…”
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8
Development of p62-Keap1 protein–protein interaction inhibitors as doxorubicin-sensitizers against non-small cell lung cancer
Published in Results in Chemistry (01-01-2022)“…Aberrant hyperactivation of nuclear factor erythroid 2-related factor 2 (Nrf2) has been reported in non-small cell lung cancer through overexpression of the…”
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Inexpensive High-Throughput Screening of Kinase Inhibitors Using One-Step Enzyme-Coupled Fluorescence Assay for ADP Detection
Published in SLAS discovery (01-03-2019)“…Protein kinases are attractive targets for both biological research and drug development. Several assay kits, especially for the detection of adenosine…”
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10
Identification of novel compounds that inhibit SnRK2 kinase activity by high-throughput screening
Published in Biochemical and biophysical research communications (22-01-2021)“…Abscisic acid (ABA) is a major phytohormone that regulates abiotic stress responses and development. SNF1-rerated protein kinase 2 (SnRK2) is a key regulator…”
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11
Structural development of 1,2,3,4-tetrahydroisoquinoline-type positive allosteric modulators of prostacyclin receptor (IPPAMs) to improve metabolic stability, and investigation of metabolic fate
Published in Bioorganic & medicinal chemistry letters (01-08-2017)“…[Display omitted] We synthesized a series of 1,2,3,4-tetrahydroisoquinoline-type positive allosteric modulators of prostacyclin receptor (IPPAMs), aiming to…”
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Synthesis of Keap1-phosphorylated p62 and Keap1-Nrf2 protein-protein interaction inhibitors and their inhibitory activity
Published in Bioorganic & medicinal chemistry letters (15-12-2016)“…[Display omitted] The Keap1-Nrf2 system is involved not only in biological defense but also in malignancy progression and chemoresistance. The…”
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13
Discovery of benzo[g]indoles as a novel class of non-covalent Keap1-Nrf2 protein-protein interaction inhibitor
Published in Bioorganic & medicinal chemistry letters (15-11-2017)“…[Display omitted] The Keap1-Nrf2 system is an attractive target for drug discovery regarding various unmet medical needs. Only covalent inhibitors for…”
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14
Restoration of Cardiac Myosin Light Chain Kinase Ameliorates Systolic Dysfunction by Reducing Superrelaxed Myosin
Published in Circulation (New York, N.Y.) (02-05-2023)Get full text
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15
Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors
Published in Chemical and Pharmaceutical Bulletin (2021)“…Mass spectrometry is a powerful methodology for chemical screening to directly quantify substrates and products of enzymes, but its low throughput has been an…”
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16
Structure–activity relationship analysis of mosquito glutathione S -transferase Noppera-bo and its inhibitors for insecticide development
Published in Acta crystallographica. Section A, Foundations and advances (02-08-2020)“…Abstract only…”
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153 - Development of Novel Inhibitors for Keap1-Nrf2 and Keap1-P62 Protein-Protein Interaction
Published in Free radical biology & medicine (01-11-2016)“…Nrf2-Keap1 system is a biological defense mechanism in response to various stressors. An inhibitor for Keap1-Nrf2 interaction to activate Nrf2 is expected as a…”
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18
Development of Novel Inhibitors for Keap1-Nrf2 and Keap1-P62 Protein-Protein Interaction
Published in Free radical biology & medicine (01-11-2016)Get full text
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Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit
Published in Bioorganic & medicinal chemistry letters (01-05-2016)“…[Display omitted] A non-selective inhibitor (1) of FMS-like tyrosine kinase-3 (FLT3) was identified by fragment screening and systematically modified to afford…”
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