Research
Faculty Members
Compound Library Screening Center Drug Discovery Screening Unit
Sakamoto JunichiSpecially Appointed Assosiate Professor
Drawing on my experience and knowledge acquired from working in pharmaceutical company and drug discovery support CRO, I aim to contribute to academic drug discovery in the areas of target selection, assay development, high-throughput screening (HTS), and compound evaluation during the pharmaceutical exploration stage.
Work Experience:
1992.04-2017.06 Takeda Pharmaceutical Company Ltd.
2017.07-2024.06 Axcelead Drug Discovery Partners Inc.
2024.07- Compound Library Screening center Graduate School of Pharmaceutical Science, Osaka University
Education:
1992.03 M.S.(Agriculture) Kyusyu University
2018.03 Ph.D (Biological Science) Tsukuba University
Research theme
Support for high-throughput screening (HTS) using a compound library
The key aspect of compound screening is obtaining hit compounds that have been confirmed to genuinely act on the target through counter assays and confirmation assays. For academic researchers aiming to acquire such compounds, we propose a screening cascade designed to identify better hit compounds. Additionally, our team can assist in constructing assay systems and performing high-throughput screening, providing comprehensive support for the entire screening process as needed.
Support for the provision of compound libraries
Selecting a library that aligns with the objectives of compound screening is crucial for obtaining better hit compounds. The Center for Supporting Drug Discovery and Life Science Research has useful Library collections for drug discovery, such as J-PUBLIC compound library, pharmaceutical company original library, Osaka university original library, and the commercial compound libraries including Drug-like and Pharmacological Diversity sets. We select, recommend, and provide suitable libraries from these collections that have a high potential for selecting hit compounds.
Support for Hit follow-up in Hit to Lead
Based on our accumulated knowledge and experience, we propose and support the validation of the mechanism of action (MOA) of hit compounds and the evaluation of analog compounds. Furthermore, the strategy for selecting lead compound candidates from the hit compounds is recommended and supported by the collaboration with our Lead Exploration unit.
Support for the Use of Drug Discovery Research Equipment
Compound library screening center is equipped with a variety of high-throughput screening and compound evaluation assay instruments for drug discovery research. We provide access to these instruments for companies, academic institutions, and non-profit organizations, with only the cost of consumables.
Representative achievements
Identification of novel inhibitors of Keap1/Nrf2 by a promising method combining protein-protein interaction-oriented library and machine learning
Y Shimizu, T Yonezawa, J Sakamoto, T Furuya, M Osawa, K Ikeda
Sci Rep. 2021 Apr 1;11(1):7420.
Discovery of an Irreversible and Cell-Active BCL6 Inhibitor Selectively Targeting Cys53 Located at the Protein-Protein Interaction Interface
T Sameshima, T Yamamoto, O Sano, S Sogabe, S Igaki, K Sakamoto, K Ida, M Gotou, Y Imaeda, J Sakamoto, I Miyahisa
Biochemistry. 2018 Feb 27;57(8):1369-1379.
Identification and Characterization of a New Series of Ghrelin O-Acyl Transferase Inhibitors
M Yoneyama-Hirozane, K Deguchi, T Hirakawa, T Ishii, T Odani, J Matsui, Y Nakano, K Imahashi, N Takakura, I Chisaki, S Takekawa, J Sakamoto
SLAS Discov. 2018 Feb;23(2):154-163.
Discovery of a Kelch-like ECH-associated protein 1-inhibitory tetrapeptide and its structural characterization
S Sogabe, K Sakamoto, Y Kamada, A Kadotani, Y Fukuda, J Sakamoto
Biochem Biophys Res Commun. 2017 May 6;486(3):620-625.
High-Throughput Quantitative Intrinsic Thiol Reactivity Evaluation Using a Fluorescence-Based Competitive Endpoint Assay
T Sameshima, I Miyahisa, S Yamasaki, M Gotou, T Kobayashi, J Sakamoto
SLAS Discov. 2017 Oct;22(9):1168-1174.
Novel DOCK2-selective inhibitory peptide that suppresses B-cell line migration
K Sakamoto, Y Adachi, Y Komoike, Y Kamada, R Koyama, Y Fukuda, A Kadotani, T Asami, J Sakamoto
Biochem Biophys Res Commun. 2017 Jan 29;483(1):183-190.
Discovery of high-affinity BCL6-binding peptide and its structure-activity relationship
K Sakamoto, S Sogabe, Y Kamada, N Sakai, K Asano, M Yoshimatsu, K Ida, Y Imaeda, J Sakamoto
Biochem Biophys Res Commun. 2017 Jan 8;482(2):310-316.
A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR) γ agonists: design and synthesis of benzylpyrazole acylsulfonamides
K Rikimaru 1, T Wakabayashi, H Abe, H Imoto, T Maekawa, O Ujikawa, K Murase, T Matsuo, M Matsumoto, C Nomura, H Tsuge, N Arimura, K Kawakami, J Sakamoto, M Funami, CD Mol, GP Snell, KA Bragstad, B Sang, DR Dougan, T Tanaka, N Katayama, Y Horiguchi, Y Momose
Bioorg Med Chem. 2012 Jan 15;20(2):714-33.
A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes
J Sakamoto, H Kimura, S Moriyama, H Imoto, Y Momose, H Odaka, H Sawada
Eur J Pharmacol. 2004 Jul 8;495(1):17-26
Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone
J Sakamoto, H Kimura, S Moriyama, H Odaka, Y Momose, Y Sugiyama, H Sawada
Biochem Biophys Res Commun. 2000, Nov 30;278(3):704-11.
