Unit Leader
Mikako Shirouzu
Ph.D.
Drug Discovery Structural Biology Platform Unit
Location Yokohama
E-mailmikako.shirouzu[at]riken.jp
Please replace [at] with @.
RIKEN Program for Drug Discovery and Medical Technology (DMP) is developing new candidate drugs and technologies for drug discovery and medical treatment. As part of the activities, our unit carries out protein sample preparation, evaluation of candidate compounds in vitro and in a cell-based manner, and structural analysis of their complexes to improve monoclonal antibody drugs, vaccines, and candidate small molecular drugs. Our activities as experts of protein science and cell biology are indispensable for the rational drug development promoted by DMP.
Project
- Preparation of antigen proteins for monoclonal antibody drugs and vaccines
- Preparation of target proteins for candidate compound evaluation and structural analysis
- In vitro compound evaluations for small molecular drugs
- Cell-based compound evaluations for small molecular drugs
- Complex structural analysis for rational drug development
Selected Publications
Takemori T, Sugimoto-Ishige A, Nishitsuji H, et al.
Establishment of a Monoclonal Antibody against Human NTCP That Blocks Hepatitis B Virus Infection.
Journal of Virology
96(5), e0168621 Wed Mar 09 00:00:00 JST 2022
doi: 10.1128/JVI.01686-21
Yamamoto H, Sakai N, Ohte S, et al.
Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva.
Bioorganic & Medicinal Chemistry Letters
38, 127858 Thu Apr 15 00:00:00 JST 2021
doi: 10.1016/j.bmcl.2021.127858
Mizuta H, Okada K, Araki M, et al.
Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer.
Nature Communications
12(1), 1261 Wed Feb 24 00:00:00 JST 2021
doi: 10.1038/s41467-021-21396-w
Nara T, Nakagawa Y, Tsuganezawa K, et al.
The ubiquinone synthesis pathway is a promising drug target for Chagas disease.
PLOS One
16(2), e0243855 Thu Feb 04 00:00:00 JST 2021
doi: 10.1371/journal.pone.0243855
Takahashi K, Akatsu Y, Podyma-Inoue KA, et al.
Targeting all transforming growth factor-β isoforms with an Fc chimeric receptor impairs tumor growth and angiogenesis of oral squamous cell cancer.
The Journal of Biological Chemistry
295(36), 12559-12572 Fri Sep 04 00:00:00 JST 2020
doi: 10.1074/jbc.RA120.012492
Sato T, Sekimata K, Sakai N, et al.
Structural Basis of Activin Receptor-Like Kinase 2 (R206H) Inhibition by Bis-heteroaryl Pyrazole-Based Inhibitors for the Treatment of Fibrodysplasia Ossificans Progressiva Identified by the Integration of Ligand-Based and Structure-Based Drug Design Approaches.
ACS Omega
5(20), 11411-11423 Tue May 26 00:00:00 JST 2020
doi: 10.1021/acsomega.9b04245
Yasukawa M, Ando Y, Yamashita T, et al.
CDK1 dependent phosphorylation of hTERT contributes to cancer progression.
Nature Communications
11(1), 1557 Wed Mar 25 00:00:00 JST 2020
doi: 10.1038/s41467-020-15289-7
Tsuganezawa K, Sekimata K, Nakagawa Y, et al.
Identification of small molecule inhibitors of human COQ7.
Bioorganic & Medicinal Chemistry
28(1), 115182 Wed Jan 01 00:00:00 JST 2020
doi: 10.1016/j.bmc.2019.115182
Sekimata K, Sato T, Sakai N, et al.
Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H).
Chemical & Pharmaceutical Bulletin
67(3), 224-235 Sun Dec 01 00:00:00 JST 2019
doi: 10.1248/cpb.c18-00598
Tanaka M, Ishige A, Yaguchi M, et al.
Development of a simple new flow cytometric antibody-dependent cellular cytotoxicity (ADCC) assay with excellent sensitivity.
Journal of Immunological Methods
464, 74-86 Tue Jan 01 00:00:00 JST 2019
doi: 10.1016/j.jim.2018.10.014