Laboratory of Physical Chemistry for Drug Design

CDK8 inhibitor KY-065 rescues skeletal abnormalities in achondroplasia model mice

Koki Sadamori, Takuya Kubo, Tomoki Yoshida, Megumi Yamamoto, Yui Shibata, Kazuya Fukasawa, Kazuya Tokumura, Tetsuhiro Horie, Takuya Kadota, Ryotaro Yamakawa, Hironori Hojo, Nobutada Tanaka, Tatsuya Kitao, Hiroaki Shirahase, Eiichi Hinoi.
Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, 1087 (3) :167626 (2025)
https://doi.org/10.1016/j.bbadis.2024.167626

The Diverse Binding Modes Explain the Nanomolar Levels of Inhibitory Activities Against 1-Deoxy-d-Xylulose 5-Phosphate Reductoisomerase from Plasmodium falciparum Exhibited by Reverse Hydroxamate Analogs of Fosmidomycin with Varying N-Substituents

Takada, Sana, Mona A. Abdullaziz, Stefan H?fmann, Talea Knak, Shin-ichiro Ozawa, Yasumitsu Sakamoto, Thomas Kurz, and Nobutada Tanaka.
Molecules, 30 (1) :72 (2024)
https://doi.org/10.3390/molecules30010072

Expanding the Chemical Space of Reverse Fosmidomycin Analogs

Talea Knak, Sana Takada, Boris Illarionov, Violetta Krisilia, Lais Pessanha de Carvalho, Beate Lungerich, Yasumitsu Sakamoto, Stefan H?fmann, Adelbert Bacher, Rainer Kalscheuer, Jana Held, Markus Fischer, Nobutada Tanaka, and Thomas Kurz.
ACS Medicinal Chemistry Letters, 16 (1) :136-143 (2024)
https://doi.org/10.1021/acsmedchemlett.4c00501

Reverse N-Substituted Hydroxamic Acid Derivatives of Fosmidomycin Target a Previously Unknown Subpocket of 1-Deoxy-d-xylulose 5-Phosphate Reductoisomerase (DXR)

Mona A Abdullaziz, Sana Takada, Boris Illarionov, Lais Pessanha de Carvalho, Yasumitsu Sakamoto, Stefan H?fmann, Talea Knak, Anna-Lene Kiffe-Delf, Flaminia Mazzone, Klaus Pfeffer, Rainer Kalscheuer, Adelbert Bacher, Jana Held, Markus Fischer, Nobutada Tanaka, Thomas Kurz.
ACS Infectious Diseases, 10 (5) :1739-1752 (2024)
https://doi.org/10.1021/acsinfecdis.4c00100

The stability of NPM1 oligomers regulated by acidic disordered regions controls the quality of liquid droplets

Mitsuru Okuwaki, Shin-Ichiro Ozawa, Shuhei Ebine, Motoki Juichi, Tadanobu Umeki, Kazuki Niioka, Taiyo Kikuchi, Nobutada Tanaka.
Journal of Biochemistry, 174 (5) :461-476 (2023)
https://doi.org/10.1093/jb/mvad061

Design and Pharmacological Chaperone Effects of N-(4'-Phenylbutyl)-DAB Derivatives Targeting the Lipophilic Pocket of Lysosomal Acid α-Glucosidase

Atsushi Kato, Izumi Nakagome, Maki Kise, Kousuke Yoshimura, Nobutada Tanaka, Robert J Nash, George W J Fleet, Yota Kobayashi, Hayato Ikeda, Takuya Okada, Naoki Toyooka.
Journal of Medicinal Chemistry, 66 (13) :9023-9039 (2023)
https://doi.org/10.1021/acs.jmedchem.3c00637

Over 40 Years of Fosmidomycin Drug Research: A Comprehensive Review and Future Opportunities

Talea Knak, Mona A. Abdullaziz, Stefan H?fmann, Leandro A. Alves Avelar, Saskia Klein, Matthew Martin, Markus Fischer, Nobutada Tanaka, Thomas Kurz.
Pharmaceuticals, 15 :1553 (2022)
https://doi.org/10.3390/ph15121553

The Stat3 Inhibitor F0648-0027 is a Potential Therapeutic Against Rheumatoid Arthritis

Yosuke Kaneko, Shin-ichiro Ozawa, Yuiko Sato, Tami Kobayashi, Tatsuaki Matsumoto, Kana Miyamoto, Shu Kobayashi, Kengo Harato, Shuichi Hirono, Morio Matsumoto, Masaya Nakamura, Yasuo Niki, Takeshi Miyamoto.
Biochemical and Biophysical Research Communications, 636 :133-140 (2022)
https://doi.org/10.1016/j.bbrc.2022.10.106

Introduction of C-alkyl branches to l-iminosugars changes their active site binding orientation

Atsushi Kato, Izumi Nakagome, Kosuke Yoshimura, Uta Kanekiyo, Mana Kishida, Kenta Shinzawa, Tian-Tian Lu, Yi-Xian Li, Robert J. Nash, George W. J. Fleet, Nobutada Tanaka, Chu-Yi Yu.
Organic & Biomolecular Chemistry, 20 (36) :7250-7260 (2022)
https://doi.org/10.1039/d2ob01099b

Synthesis and Evaluation of Habiterpenol Analogs

Miyuki Konya, Shiho Arima, Daiki Lee, Masaki Ohtawa, Kenta Shimoyama, Takashi Fukuda, Ryuji Uchida, Hiroshi Tomoda, Noriyuki Yamaotsu, Nobutada Tanaka, Tohru Nagamitsu.
Chemical and Pharmaceutical Bulletin, 70 (4) :261-268 (2022)
https://doi.org/10.1248/cpb.c21-00993