Skill Development for Lead Discovery

Numbering Code G-PHA02 75102 PJ86 Year/Term 2021 ・ Irregular, year-round
Number of Credits 4 Course Type Practical training
Target Year 1st and 2nd year master's students Target Student
Language Japanese Day/Period
Instructor name KAKEYA HIDEAKI (Graduate School of Pharmaceutical Sciences Professor)
OHNO HIROAKI (Graduate School of Pharmaceutical Sciences Professor)
HATTORI AKIRA (Graduate School of Pharmaceutical Sciences Associate Professor)
INUKI SHINSUKE (Graduate School of Pharmaceutical Sciences Associate Professor)
KURANAGA TAKEFUMI (Graduate School of Pharmaceutical Sciences Assistant Professor)
Arichi Norihito (Graduate School of Pharmaceutical Sciences Assistant Professor)
Outline and Purpose of the Course This course outlines search methods and activity evaluation methods for pharmaceutical lead compounds, identification methods for target molecules, and chemical synthesis methods. It also introduces the latest findings on peripheral technologies that enable these methods and uses all of this as a springboard for discussion.
Through presentations and associated discussions, this course aims to teach students the experiment skills needed to search for the lead compounds in drug discovery (including compound screening and drug synthesis) and carry out molecular design, as well as associated teaching methods.
Course Goals To understand and develop the ability to explain the latest knowledge and skills concerning search methods for pharmaceutical lead compounds, design and synthesis methods, and target molecule identification methods, and to develop presentation skills.
Schedule and Contents It is intended that each of the following subjects will occupy 2 weeks of classes:

1. Introduction
2-3. Develop skills related to establishing screening methods for lead compounds
・Skill development and presentations related to establishing screening methods for lead compounds, with associated discussion and commentary
4-5. Develop skills related to isolating and determining the structure of lead compounds from natural resources
・Skill development and presentations related to isolating and determining the structure of lead compounds from natural resources, with associated discussion and commentary
6-7. Develop skills related to the structure-activity relationship and optimization research on lead compounds
・Skill development and presentations related to the structure-activity relationship and optimization research on lead compounds, with associated discussion and commentary
8-9. Develop skills related to the identification and evaluation of pharmaceutical molecular targets
・Skill development and presentations related to the identification and evaluation of pharmaceutical molecular targets, with associated discussions and commentary
10-11. Develop skills related to the use of compound databases and compound libraries
・Skill development and presentations related to the use of compound databases and compound libraries, with associated discussions and commentary
12-13. Develop skills related to drug discovery research on bioactive peptides
・Skill development and presentations related to drug discovery research on bioactive peptides, with associated discussions and commentary
14-15. Develop skills related to solid-state synthesis and combinatorial chemistry
・Skill development and presentations related to solid-state synthesis and combinatorial chemistry, with associated discussions and commentary
Evaluation Methods and Policy Students will be comprehensively evaluated based on attendance and input in presentations and discussions.
Course Requirements Attendance of introduction to drug discovery and organic chemistry
Study outside of Class (preparation and review) Students should proactively prepare in advance and review class content, and should also aim to develop basic knowledge and establish a research activity skill base.
Textbooks Textbooks/References Others; printouts will be distributed where appropriate.
References, etc. Inshiriko Souyaku Kagaku: Genomu Jouhou kara Souyaku he, (Kyoto Hirokawa Shoten, 2010) ISBN:9784901789035. Seibutsu Kassei Bunshi no Kemikaru Baiorojii, (Kagaku Doujin, 2016) ISBN:9784759813791. Toppudoraggu kara Manabu Souyaku Kagaku, (Tokyo Kagaku Doujin, 2012) ISBN:9784807907762. Academic journals in the fields of chemistry and biology, including Nature, Science, J. Am. Chem. Soc., Ang. Chem. Int. Ed.
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