RIKEN Program for Drug Discovery and Medical Technology Platforms


Drug Discovery and Medical Technology Platforms to Support One-Stop, Speedy Research and Development

 Wide-ranging technology platforms are necessary for the research and development of new drugs and medical technologies, and the technology platforms themselves are also innovating in step with progress in life science research. In drug discovery research, we create the seeds for drug discovery through a range of screenings including identification and analysis of the proteins that cause diseases and other drug discovery targets, aiming for optimization through medicinal chemistry and then proceeding to preclinical trial. Consequently, in drug discovery and medical technology research, the work is not concluded by a single research laboratory, but it is advanced by organizational strategy directing a wide range of technology platforms. The Drug Discovery and Medical Technology Platforms have responded by structuring each drug discovery platform unit and rebuilding the drug discovery research functions already extant at the RIKEN BASE (Bioinformatics And Systems Engineering) Division which studies the life science within RIKEN Yokohama Institute.

 We have pinpointed three research and development domains for implementing drug discovery and medical technology. As well as upgrading and structuring these domains we are taking steps for collaborative measures with external organizations. They are the basic research domain for identifying and analyzing drug discovery targets, the investigative research and development domain for screening and optimizing compounds, and the TR (translational) support domain for clinical studies and for the preclinical studies that conduct safety and security evaluations in order to advance to the stage of clinical studies (See diagram below).

 At the Drug Discovery and Medical Technology Platforms, we are in charge of updating compound libraries, the explorative research and development areas in the basic research domain including interactive and structural analysis of complexes, as well as the function of building bridges to the TR support domain.

 To cover these research and development domains, we have established seven drug discovery units and four cutting-edge training platforms, and we have outsourced the technology platforms that do not exist within the research institute. With respect to the TR support domain, we are collaborating with the Tohoku University School of Medicine and others.


Platform Unit Clusters and Cutting-Edge Training Platforms for Drug Discovery and Medical Technology
-Building a Network of Practical Technology Platforms and Promoting R&D-

 To support the research and development domains for implementing drug discovery and medical technology, we have established the cutting-edge training platforms and the Drug Discovery and Medical Technology Platform Units listed below. In addition to basic functions such as supporting drug discovery research, each platform unit is evolving proprietary technologies and know-how, and building technology platforms network that are unique to the Drug Discovery and Medical Technology Platforms.

Chemical Bank Platform Unit

 The forte of the Chemical Bank Unit is the 24,000 natural compounds collected in the NPdepo natural compound depository, and its database. As well as independently collecting and storing microbial secondary metabolites, the Bank promotes the depository of natural compounds by making the database of compounds available to the public on the Internet. In addition, the Bank is undertaking screening research for interaction between natural compounds and proteins by developing and using a chemical chip capable of detecting and measuring trace amounts.>>Details can be found here

>Drug Discovery Computational Chemistry Platform Unit

 At the Drug Discovery Computational Chemistry Platform Unit, we implement high-precision in silico screening through the latest in both modeling theories and statistical theories, using the three-dimensional structure of target proteins and information about known inhibitors. Our strong points are machine learning of experimental data such as the results of WET screening, and facilitating optimized designs for ADMET etc.
>>Details can be found here

Drug Discovery Structural Biology Platform Unit

 The Crystallographic Drug Discovery Platform Unit fulfills the role of a core platform for drug discovery research based on three-dimensional analysis of proteins. The unit obtains sample preparations of target proteins, crystallization and x-ray diffraction data, conducts high-throughput three-dimensional structural analysis, quickly and accurately obtaining information on the three-dimensional structure of target proteins and the bonding state of candidate compounds for drugs.>>Details can be found here

Drug Discovery Chemistry Platform Unit

 The Drug Discovery Chemistry Platform aims to move to the next stage of research and development based on medicinal chemistry. Specifically, the unit aims to identify candidate compounds for development by promoting the synthesis of new pharmaceutical candidate compounds having pharmacological activity toward the target, and structure activity-related research based on pharmacological and drug metabolizing/pharmacokinetic assay data. By developing Fragment-Based Drug Discovery (FBDD) as a method for discovering seeds and lead compounds in the initial stages of explorative research of promising pharmaceutical compounds, the platform also aims to identify new drug discovery seeds and lead compounds through collaboration with the drug discovery platform.>>Details can be found here

Drug Discovery Imaging Platform Unit

 At the Drug Discovery Imaging Platform Unit, we are advancing in vivo pharmacokinetic research of marmosets (monkeys), mice and humans by utilizing molecular imaging technology focused on positron emission tomography (PET). Labeling technologies for molecular imaging probes guarantee in vivo observation time and improve tracing after metabolic breakdown. Also, with a view to clinical studies of microdoses, we aim to build new drug discovery processes, developing labeling and probes for drug candidate compounds, as well as utilizing mice-to-human streamlined molecular imaging techniques.>>Details can be found here

Leading Computational Science Platform Unit
Leading Computational Science Platform Unit:
Using Supercomputers for Advanced In Silico Screening Technologies Including Molecular Behavior

 This unit aims for "the establishment and application of in silico drug discovery by means of leading computational technologies using large-scale, high-speed supercomputers" in order to promote drug discovery research. We implement simulation technologies to predict high-precision binding affinity, taking into account the dynamics of the complex structures of protein/low molecular compounds in aqueous solution in order to develop a high level of precision for in silico drug discovery. This is useful for deepening understanding and investigations at the molecular level of drug candidate compounds, and for specifying structural formula for promising compounds (production and selection).

Seed Compounds Exploratory Unit for Drug Discovery Platform

 This Unit aims to explore seed compounds for drug discovery by High-Throughput Screening(HTS). We also work for assay development, adaptation of assay methods for HTS, and evaluation and profiling of hit compounds of HTS as well as HTS.>>Details can be found here

in preparation

 in preparation


Cutting-Edge Training Platforms to Improve Development Support for Drug Discovery and Medical Technologies
-Toward Innovation in Research and Development through New Technologies-


Next Generation Sequence Platform:

 At the Next Generation Sequence Unit, we are preparing advanced next-generation sequencers with the Cell Innovation Program at the Ministry of Education as the sequence base, and we are developing utilization technologies. Not simply a department for technical support and developing utilization technologies, the unit undertakes cutting-edge bioscience research and verifies the validity of the research methods. In RNA analysis, in particular, the unit has contributed to future drug discovery research on the basis of outstanding results such as detecting large amounts of non-coding RNA and producing a full-length cDNA library (mouse, Arabidopsis etc.)
>>Details can be found here

Cellular Imaging Platform

 At the Cellular Imaging Platform, we analyze intracellular distribution and behavior (temporal/ spatial control) in the important biomolecules controlling vital phenomena, such as propagation and differentiation, through cellular imaging by labeling the targeted biomolecules with fluorescence, which emits light, and tracking their movements. By using several fluorescent proteins, it is also possible to simultaneously observe the behavior of important biomolecules (multi-color imaging) in complex systems such as cell cycle analysis or intracellular signaling. Analysis of real-time changes in target proteins and intracellular information in response to pharmaceuticals is expected to be useful for drug discovery research.
>>Details can be found here