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Research

Research

BDR researchers coming from diverse research fields are working together to achieve higher goals.

Seminars & Symposia

Seminars & Symposia

BDR hosts annual symposium and regular seminars inviting international scientists in life science.

Careers & Study

Careers & Study

BDR embraces people from diverse backgrounds, and strives to create an open and supportive setting for research.

Outreach

Outreach

BDR communicates the appeal and significance of our research to society through the use of various media and activities.

News

News

From research, events, people and everything in between, find out what’s going on at RIKEN BDR.

About Us

About Us

Exploring the scientific foundations of life through interdisciplinary approaches to address society’s problems.

Photo of Unit leder, Mikako Shirouzu

Unit Leader
Mikako Shirouzu Ph.D.

Drug Discovery Structural Biology Platform Unit

Location Yokohama

E-mailmikako.shirouzu[at]riken.jp

Please replace [at] with @.

Evaluation of candidate compounds and analysis of their complex structures for DMP activities.

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.

Image of research summary

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

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 (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 (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 (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 (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 (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 (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 (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 (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 (2019) doi: 10.1016/j.jim.2018.10.014

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