Drug Discovery & Development II: Lead Discovery Technology

Numbering Code G-PHA02 61111 LJ86 Year/Term 2022 ・ Irregular, Second semester
Number of Credits 2 Course Type Lecture
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)
TAKASU KIYOSEI (Graduate School of Pharmaceutical Sciences Professor)
TAKAKURA YOSHINOBU (Graduate School of Pharmaceutical Sciences Professor)
Outline and Purpose of the Course (Purpose) The aim is to deepen understanding of cutting-edge research in interdisciplinary areas spanning chemistry and biology, and to acquire knowledge and theory on the molecular design and chemical synthesis techniques of compounds mainly used for drug discovery and the basic technology for evaluating the bioactivity of compounds.
(Overview) The most recent topics regarding study and technology related to the identification of lead compounds for drug discovery will be introduced, and the basic technologies related to the supply of compounds essential for the identification of lead compounds and their theories will be lectured focusing on organic synthetic chemistry, drug discovery, and natural product chemistry. The paper also introduces the technologies of molecular biology and cell biology related to the evaluation of compounds and the utilization of information obtained from genome-related science and screening, and outlines a series of processes related to lead compound search.
Course Goals ・Acquire the fundamentals of chemical synthesis technology used in drug lead identification.
・Acquire the fundamentals of molecular design using various compounds.
・Deepen understanding of the bioactivity evaluation of compounds.
・Learn and understand the latest technologies and trends in drug discovery research.
Schedule and Contents 1st to 5th Classes
Basis and Application of Chemical Synthesis Technologies for Compounds Used in Drug Lead Identification
・Introduction to Synthetic Methods Used in Drug Discovery Research
・Molecular Design and Efficient Synthetic Methods for Compounds with Suitable Properties as Pharmaceuticals
・Theory and Application of New Chemical Synthesis Technologies to Realize Efficient Structure Optimization Study
・Molecular Design and Drug Discovery from Nuclear Acids, Fatty Acids, and Sugars
・Molecular Design and Drug Discovery from Amino Acids, Peptides, and Proteins

6th to 10th Classes
Natural-Product-Based Drug Discovery and Chemical Biology Research
・Technologies for the Separation and Structure Determination of Naturally-Originated Compounds Including Secondary Metabolites
・Examples of Drug Discovery Practices from Naturally Originated Compounds
・Bioactivity Evaluation Based on Cell Functioning
・Bioactivity Evaluation Based on Cell and Tissue Representation

11th to 14th Classes
Drug Discovery Research in Practice
・Identification of Enzyme-Targeting Compounds and Their Applications
・Identification of Receptor-Targeting Compounds and Their Applications
・Identification of Compounds Targeting Ion Channels and Other Biomolecular Entities and Their Applications
・Overview of Compound Libraries and Their Practices in Drug Discovery
・Utilization of Databases in Drug Leads Identification

15th Class
Supplementary Lecture and General Discussion
Evaluation Methods and Policy Comprehensively evaluated based on attendance at lectures, class notes (50%), and reports assigned during lectures (50%).
Course Requirements None
Study outside of Class (preparation and review) It is recommended that students review the undergraduate level content of the relevant items before the class.
After the classes, do independent study on items of interest and prepare reports.
Textbooks Textbooks/References Printouts will be distributed if otherwise necessary.
References, etc. Other texts may be designated depending on the content of the lecture.
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