Atsunori Kaneshige 11th Annual Conference of the International Chemical Biology Society 2022

Atsunori Kaneshige

Atsunori Kaneshige, PhD Email: atsunori@umich.edu Tel: 734-210-2160 Address: 1431 McIntyre St, Ann Arbor, MI, 48105, USA EDUCATION PhD, Department of Medicinal Chemistry, University of Michigan, USA 2022 Title: “Development of a First-In-Class STAT5 PROTAC Degrader” Thesis Link: https://dx.doi.org/10.7302/5901, Advisor: Professor Shaomeng Wang MBA, Ross School of Business, University of Michigan, USA 2016 MS, Faculty of Pharmaceutical Sciences, Kyoto University, Japan 2009 BS, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan 2006 PROFESSIONAL RESEARCH TRAINING Medicinal/Process Chemist, Otsuka Pharmaceutical Co., Ltd., Japan CMC Team Leader 2014 – 2015 Bulk Pharmaceutical Chemicals Dept., Otsuka Pharmaceutical Co., Ltd. • Coinventor on patent (PCT/JP2015/004371) for drug candidate, OPC-167832 • Kilogram scale manufacturing of OPC-167832 Lead Medicinal Chemistry Researcher 2010 – 2014 Bulk Pharmaceutical Chemicals Dept., Otsuka Pharmaceutical Co., Ltd. • Contributed to the tuberculosis drug discovery project from its early medicinal chemistry stage • Contributed to the discovery of OPC-167832 for the treatment of tuberculosis, which advanced to the pre-clinical and clinical evaluation phase. Junior Researcher 2009 – 2010 Bulk Pharmaceutical Chemicals Dept., Otsuka Pharmaceutical Co., Ltd. • Trained as a medicinal chemist in tuberculosis drug discovery project • Trained as a process chemist though the manufacturing of Aripiprazole (Abilify) at ton-scale in Otsuka’s GMP production factories. ACADEMIC RESEARCH TRAINING Graduate Student Research Assistant 2016 – 2022 Department of Medicinal Chemistry, University of Michigan • Discovered First-In-Class Selective and Efficacious STAT5 degraders • Discovered First-In-Class Selective and Efficacious STAT6 degraders • Filed patents for START5/6 inhibitors and STAT5/6 degraders • Designed and synthesized >2,000 small molecules with organic chemistry knowledge and skill • Cultured and maintained > 40 hematologic and solid cancer cell lines • Performed cell viability assays to determine IC50 values • Performed western blotting analyses to determine DC50 values • Performed fluorescence polarization assay to determine Ki values • Contributed to multi-disciplinary project that requires organic synthesis, binding assay development, in vitro and in vivo evaluation, pharmacokinetic and pharmacodynamic evaluation, and cocrystal structures of molecules in complex with proteins. RESEARCH INTERESTS • Targeting “undruggable”, or “difficult-to-drug” proteins by chemical tools to study cancer biology, immunology, and allergy, with the goal of therapeutics development. • Development of new chemical biology platform with which to answer biological questions and to provide new strategies for therapeutics development • Investigation of new modalities for diseases that otherwise would not be treated by traditional small molecules. REVISED MANUSCRIPTS UNDER CONSIDERATION “A Potent and Selective Small-Molecule STAT5 PROTAC Degrader Capable of Achieving Tumor Regression In Vivo” Atsunori Kaneshige, Longchuan Bai, Mi Wang, Donna McEachern, Jennifer Lynn Meagher, Renqi Xu, Wei Jiang, Yu Wang, Hoda Metwally, Paul Kirchhoff, Hui Jiang, Bo Wen, Duxin Sun, Jeanne Stuckey, and Shaomeng Wang (at Nature Chemical Biology) MANUSCRIPTS READY TO BE SUBMITTED “Structure-Guided Discovery of a Potent, Selective, and Efficacious STAT5 PROTAC Degrader” Atsunori Kaneshige, Longchuan Bai, Mi Wang, Donna McEachern, Jennifer Lynn Meagher, Renqi Xu, Wei Jiang, Yu Wang, Hoda Metwally, Paul Kirchhoff, Bo Wen, Duxin Sun, Jeanne Stuckey, and Shaomeng Wang MANUSCRIPTS UNDER PREPARATION “Structure-Guided Discovery of a Potent, Selective, and Efficacious STAT6 PROTAC Degrader” Atsunori Kaneshige, Longchuan Bai, Mi Wang, Donna McEachern, Jennifer Lynn Meagher, Renqi Xu, Paul Kirchhoff, Bo Wen, Duxin Sun, Jeanne Stuckey, and Shaomeng Wang PATENTS • STAT5 and STAT6 inhibitors and uses thereof 2022 • STAT5 and STAT6 degraders and uses thereof 2022 • Heterobicyclic compounds and their use for the treatment of tuberculosis. 2018 U.S. Patent 10,053,446. PUBLICATIONS Yamamoto, Y., Yamaguchi, T., Kaneshige, A., Hashimoto, A., Kaibe, S., Miyawaki, A., 2017 Yamada, K.I. and Tomioka, K., 2017. Consecutive Aminolithiation–Carbolithiation of a Linear Aminoalkene Bearing Terminal Vinyl Sulfide Moiety to Give Hydroindolizine. Synlett, 28(20), pp.2913-2917. Tsuchida, S., Kaneshige, A., Ogata, T., Baba, H., Yamamoto, Y. and Tomioka, K., 2008 2008. Consecutive Cyclization of Allylaminoalkene by Intramolecular Aminolithiation − Carbolithiation. Organic Letters, 10(16), pp.3635-3638. Ogata, T., Ujihara, A., Tsuchida, S., Shimizu, T., Kaneshige, A. and Tomioka, K., 2007 2007. Catalytic asymmetric intramolecular hydroamination of aminoalkenes. Tetrahedron Letters, 48(38), pp.6648-6650. SKILLS IN EXPERIMENT • Organic synthesis from small scale synthesis to production scale synthesis • Fluorescence Polarization Assay Development to measure binding affinities of molecules • Western Blotting Analysis to quantify protein levels • Luminescent Cell Viability Assay (CellTiter-Glo) SKILLS IN SOFTWARE • NMR analysis • ChemDraw • GraphPad Prism • Endnote • Microsoft Office • Tecan Microplate Readers SKILLS IN PROGRAMMING (as a side interest) Python programming, especially familiar with Machine Learning Algorithms • My Github repository: https://github.com/NoriKaneshige • My test program called PDB_ZINC_SCRAPER: https://github.com/NoriKaneshige/PDB_ZINC_SCRAPER/blob/master/README.md • My test program called Predicting_Scalar_Coupling_Constant_By_LightGBM https://github.com/NoriKaneshige/Predicting_Scalar_Coupling_Constant_By_LightGBM/blob/master/README.md