Search Results - "Doi, Satoki"
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Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders
Published in Journal of medicinal chemistry (09-07-2020)“…Dermatologic disorders such as atopic dermatitis arise from genetic and environmental causes and are complex and multifactorial in nature. Among possible risk…”
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Broad Antiretroviral Activity and Resistance Profile of the Novel Human Immunodeficiency Virus Integrase Inhibitor Elvitegravir (JTK-303/GS-9137)
Published in Journal of Virology (01-01-2008)“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Discovery of Conformationally Constrained Tetracyclic Compounds as Potent Hepatitis C Virus NS5B RNA Polymerase Inhibitors
Published in Journal of medicinal chemistry (30-11-2006)“…We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to…”
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4
Fragment-Based Discovery of Novel VE-PTP Inhibitors Using Orthogonal Biophysical Techniques
Published in Biochemistry (Easton) (18-07-2023)“…Tyrosine phosphorylation is an essential post-translational modification that regulates various biological events and is implicated in many diseases including…”
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Fragment-based lead discovery to identify novel inhibitors that target the ATP binding site of pyruvate dehydrogenase kinases
Published in Bioorganic & medicinal chemistry (15-08-2021)“…[Display omitted] A fragment-based lead discovery approach was applied to Pyruvate Dehydrogenase Kinases (PDHKs) to discover inhibitors against the ATP binding…”
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The discovery of 3,3-dimethyl-1,2,3,4-tetrahydroquinoxaline-1-carboxamides as AMPD2 inhibitors with a novel mechanism of action
Published in Bioorganic & medicinal chemistry letters (15-01-2023)“…[Display omitted] AMP deaminase 2 (AMPD2) has been thought to play an important role in energy homeostasis and immuno-oncology, while selective AMPD2…”
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Discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by the use of docking models
Published in Bioorganic & medicinal chemistry letters (01-01-2019)“…[Display omitted] •A novel series of azetidine scaffold were identified as colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors.•Compound 4a showed…”
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Discovery of Second Generation RORγ Inhibitors Composed of an Azole Scaffold
Published in Journal of medicinal chemistry (14-03-2019)“…Starting from a previously reported RORγ inhibitor (1), successive efforts to improve in vivo potency were continued. Introduction of metabolically beneficial…”
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Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors
Published in Bioorganic & medicinal chemistry (15-12-2021)“…[Display omitted] Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. In this report, we…”
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Ternary crystal structure of human RORγ ligand-binding-domain, an inhibitor and corepressor peptide provides a new insight into corepressor interaction
Published in Scientific reports (26-11-2018)“…Retinoic acid-related orphan receptor gamma (RORγ) plays pivotal roles in autoimmune diseases by controlling the lineage of interleukin 17 (IL-17)-producing…”
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SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor
Published in ACS medicinal chemistry letters (14-01-2016)“…A novel series of RORγ inhibitors was identified starting with the HTS hit 1. After SAR investigation based on a prospective consideration of two drug-likeness…”
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Ternary complex of human ROR[gamma] ligand-binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment
Published in Genes to cells : devoted to molecular & cellular mechanisms (01-06-2017)“…Retinoid-related orphan receptor gamma (ROR[gamma]) directly controls the differentiation of Th17 cell and the production of interleukin-17, which plays an…”
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Ternary complex of human RORγ ligand‐binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment
Published in Genes to cells : devoted to molecular & cellular mechanisms (01-06-2017)“…Retinoid‐related orphan receptor gamma (RORγ) directly controls the differentiation of Th17 cell and the production of interleukin‐17, which plays an integral…”
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SAR Exploration Guided by LE and Fsp3: Discovery of a Selective and Orally Efficacious RORγ Inhibitor
Published in ACS medicinal chemistry letters (14-01-2016)“…A novel series of RORγ inhibitors was identified starting with the HTS hit 1. After SAR investigation based on a prospective consideration of two drug-likeness…”
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15
SAR Exploration Guided by LE and Fsp 3 : Discovery of a Selective and Orally Efficacious RORγ Inhibitor
Published in ACS medicinal chemistry letters (14-01-2016)Get full text
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