Výsledky vyhledávání - "Michiko Tawada"

Discovery of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization

Autor: Richard Tjhen, Noriko Uchiyama, Michiko Tawada, Yohei Kosugi, Satoshi Endo, Huikai Sun, Kei Masuda, Makoto Fushimi, Tatsuki Koike, Weston Lane

Publikováno v: Journal of Medicinal Chemistry. 64:1103-1115

O-GlcNAcase (OGA) has received increasing attention as an attractive therapeutic target for tau-mediated neurodegenerative disorders; however, its role in these pathologies remains unclear. Therefore, potent chemical tools with favorable pharmacokine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3d202dd30fc9d83817cf7c025a625af2
https://doi.org/10.1021/acs.jmedchem.0c01712

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Identification of a selective DDX3X inhibitor with newly developed quantitative high-throughput RNA helicase assays

Autor: Toshio Tanaka, Tomohiro Kawamoto, Satoshi Endo, Samuel Aparicio, Michiko Tawada, Atsushi Nakanishi, Momoko Ohori, Douglas R. Cary, Masahiro Ito, Masahiro Nogami, Toshihiro Imaeda, Misa Iwatani, Shinsuke Araki, Shoichi Nakao, Yasuhiro Imaeda

Publikováno v: Biochemical and Biophysical Research Communications. 523:795-801

The DEAD-box family of RNA helicases plays essential roles in both transcriptional and translational mRNA degradation; they unwind short double-stranded RNA by breaking the RNA-RNA interactions. Two DEAD-box RNA helicases, eukaryotic translation init

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f92b4a687affd66801c43aa881d530cd
https://doi.org/10.1016/j.bbrc.2019.12.094

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Identification of 2,6-Disubstituted 3H-Imidazo[4,5-b]pyridines as Therapeutic Agents for Dysferlinopathies through Phenotypic Screening on Patient-Derived Induced Pluripotent Stem Cells

Autor: Akiko Oki, Katsunori Sasa, Hiroyuki Takada, Bunnai Saito, Kazumasa Miyamoto, Tomoko Nagino, Hidetoshi Sakurai, Ryuichi Tozawa, Tatsuo Oikawa, Makoto Miyamoto, Yuko Kokubu, Michiko Tawada, Tomoya Sameshima, Akira Kaieda

Publikováno v: Journal of Medicinal Chemistry. 62:9175-9187

Dysferlinopathies, which are muscular diseases caused by mutations in the dysferlin gene, remain serious medical problems due to the lack of therapeutic agents. Herein, we report the design, synthesis, and structure-activity relationships of a 2,6-di

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f9111b391e088e8dd74adcaa24e72217
https://doi.org/10.1021/acs.jmedchem.9b01100

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Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554

Autor: Akiyoshi Tani, Yoshio Yamamoto, Takuo Kosaka, Tomoko Asakawa, Yasufumi Miyamoto, Tohru Yamashita, Yoshihiro Banno, Shigetoshi Tsubotani, Satoru Oi, Michiko Tawada, Hironobu Maezaki, Nobuhiro Suzuki, Koji Ikedo

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 27:3565-3571

We report a design strategy to obtain potent DPP-4 inhibitors by incorporating salt bridge formation with Lys554 in the S1′ pocket. By applying the strategy to the previously identified templates, quinoline 4 and pyridines 16a, 16b, and 17 have bee

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7cf31b4c4cb0290855e26a1afe7d7ac3
https://doi.org/10.1016/j.bmcl.2017.05.048

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Discovery of Novel and Potent Stearoyl Coenzyme A Desaturase 1 (SCD1) Inhibitors as Anticancer Agents

Autor: Hironobu Maezaki, Kouji Ono, Ikuo Miyahisa, Megumi Hirayama, Masako Sasaki, Michiko Tawada, Imamura Keisuke, Ryuichi Nishigaki, Naoki Tomita, Kazuko Yonemori, Noriyuki Nii, Yoshihiko Satoh, Yoshinori Satomi, Yoshiteru Ito, Yukiko Yamamoto, Tohru Miyazaki, Youichi Kawakita, Hiroyuki Sumi

Publikováno v: Bioorganic & Medicinal Chemistry. 25:3768-3779

A lead compound A was identified previously as an stearoyl coenzyme A desaturase (SCD) inhibitor during research on potential treatments for obesity. This compound showed high SCD1 binding affinity, but a poor pharmacokinetic (PK) profile and limited

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff5cb8ec02596711f9513a83839e2a85
https://doi.org/10.1016/j.bmc.2017.05.016

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