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2023　Design of Bioactive Molecules

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Academic unit or major
Graduate major in Life Science and Technology
Instructor(s)
Nakamura Hiroyuki  Hata Takeshi  Fujie Toshinori  Kamiya Mako  Kawai Kiyohiko 
Class Format
Lecture    (Livestream)
Media-enhanced courses
Day/Period(Room No.)
Mon3-4()  Thr3-4()  
Group
-
Course number
LST.A405
Credits
2
Academic year
2023
Offered quarter
2Q
Syllabus updated
2023/6/9
Lecture notes updated
-
Language used
English
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Course description and aims

This course describes the advanced applications of organic chemistry and the use of polymeric materials, with a review of their fundamentals and their position in bioscience and biotechnology, and the handling of biologically active molecules. Specifically, classification of biologically active molecules and expression of their activity will be discussed. In addition, metabolic mechanisms of drugs, design and chemical synthesis of drugs, fundamentals and applications of chemical biology, biomaterial polymers, and medical applications of light and radiation will be explained. In the last four lectures, an original research article(s) regarding the course topics is selected and studied, and subsequently it will be the subject of the final report.
The course promotes the integration and operationalization of basic knowledge of organic chemistry, a more advanced and cross-cutting understanding of bioactive molecules, and practical knowledge of the use of polymeric materials as well as the application of organic chemistry. In other words, students will learn about the origin, pharmacological activity, metabolism, molecular design, structure-activity relationships of natural bioactive compounds and artificial pharmaceuticals, and other important organic chemistry-centered topics, as well as chemical biology, biomaterial polymers, and medical applications of light and radiation, from a broad perspective of bioscience and pharmaceutical sciences. The objective is to organize and acquire knowledge from a broad perspective, including the positioning of these topics in the biological sciences and engineering and their relevance to pharmaceutical sciences. In the last four classes, students read recent original papers related to the course content to practically consolidate the above knowledge and ideas.

Student learning outcomes

By the end of this course, students will be able to:
1. Understand and explain the purpose and significance of design of bioactive molecules
2. Understand and explain the metabolism of pharmaceutical drugs and their molecular modification
3. Understand and explain the structure-activity relationship and synthetic design of drugs
4. Understand the concept of chemical biology, and explain the visualization and control by chemical tools
5. Understand and explain the design and fabrication methods of macromolecular biomaterials
6. Understand and explain basic chemical reactions in medical applications of photochemistry and radiation chemistry
7. Catch up the most recent trends in the design and synthesis of bioactive molecules

Keywords

pharmaceutical drug, organic chemistry, organic synthesis, drug metabolism, structure-activity relationship, medicinal chemistry, chemical biology, chemical tool, polymer chemistry, biomaterials science, biomedical engineering, photochemistry, photosensitizer, radiation chemistry

Competencies that will be developed

✔ Specialist skills Intercultural skills Communication skills Critical thinking skills Practical and/or problem-solving skills

Class flow

Lectures will be given online (Zoom), using materials distributed in advance by the faculty. A small exercise will be given in the last 10 minutes of each lecture. In the 11th through 14th lectures, students will read recent original papers related to each lecture topic and prepare a final report based on them, which will be submitted by the designated due date.

Course schedule/Required learning

  Course schedule Required learning
Class 1 Introduction: The purpose and significance of design of bioactive molecules Understand and explain the purpose and significance of design of bioactive molecules from the standpoint of organic and pharmaceutical chemistry.
Class 2 Drug metabolism Understand and explain the important chemical reactions in drug metabolism that should be considered for pharmaceutical drug design.
Class 3 Design and synthesis of pharmaceutical drugs (1) Understand and explain biomolecules as targets of drug development, interactions between drug and target biomolecules, and bioactivities.
Class 4 Design and synthesis of pharmaceutical drugs (2) Understand and explain the manipulation of organic molecules for drug development.
Class 5 Medical applications of photoirradiation and radiation (basic) Understand and explain basic chemical reactions in medical applications of photochemistry and radiation chemistry.
Class 6 Medical applications of photoirradiation and radiation (application) Understand and explain the mechanism of action of photosensitizers and radiosensitizers used in photo dynamic therapy and radiation therapy.
Class 7 Basics of chemical biology Understand the concept of chemical biology, and explain the visualization and control by chemical tools.
Class 8 Application of chemical biology Understand and explain the biological/medical application of chemical tool.
Class 9 Polymeric biomaterials (Fabrication） Understand and explain the design and fabrication of polymeric biomaterials including surface modification, microfabrication and instrumental analysis.
Class 10 Polymeric biomaterials (Application） Understand and explain the medical application of biomaterials (tissue engineering, cell therapy, organ-on-a-chip, biodevice).
Class 11 Reading of the latest research articles-1 (Pharmaceutical drug design) Learn the frontiers of the diversification of modalities in drug discovery research and cultivate practical skills for future drug development.
Class 12 Reading of the latest research articles-2 (Synthesis and bioassay of pharmaceutical drugs) Learn the frontiers of the drug synthesis including the relationship between structure and pharmacological action and acquire practical skills of the drug design.
Class 13 Reading of the latest research articles-3 (Chemical tool) Learn the frontiers of latest development of chemical tools and cultivate practical skills of the design and application of chemical tools.
Class 14 Reading of the latest research articles-4 (Utilization of polymer) Learn the frontiers of the advanced medicine utilizing functional polymers and acquire practical skills of the design of biomaterials.

Out-of-Class Study Time (Preparation and Review)

To enhance effective learning, students are encouraged to prepare and review for each class with referring to the course material.

Textbook(s)

Course materials are provided.

Reference books, course materials, etc.

If necessary, references are shown in class.

Assessment criteria and methods

Students will be assessed on the concise exercise problems in each class (40%) and the final four reports (60%). In the final reports, students’ unique interpretation and proposal to the article(s) studied in the class are welcome.

Related courses

  • LST.A402 ： Organic and Bioorganic Chemistry

Prerequisites (i.e., required knowledge, skills, courses, etc.)

No prerequisites.

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