COURSE OUTLINE: BS3013

Course Title

Drug Discovery and Development, Biotechnology

Course Code

BS3013

Offered Study Year 3, Semester 2
Course Coordinator Liu Chuan Fa (Assoc Prof) cfliu@ntu.edu.sg 6316 2867
Pre-requisites BS1003 & BS2004 OR BS1013 & BS2004
AU 3
Contact hours Lectures: 24, Tutorials: 12
Approved for delivery from
Last revised 16 Dec 2022, 13:30

Course Aims

This course is designed to tackle one of the most important issues in healthcare – the discovery and development of safe and effective drugs against diseases such as cancer, diabetes, neurological disorders and viral infections as well as for disease prevention and health improvement. It aims to equip you with the knowledge and skills that are in great need in the pharmaceutical and biotechnology industry. This is an interdisciplinary course, combining chemistry with biology and pharmacology and dealing with both small-molecule drugs and biologics. It covers the basic concepts and principles of the three phases of drug action (pharmaceutics, pharmacokinetics and pharmacodynamics), the techniques and methods used in drug discovery and development (target identification and validation, lead discovery and optimization, preclinical and clinical trials), and specific topics on drugs acting on different classes of drug targets.

Intended Learning Outcomes

Upon successfully completing this course, you should be able to:

  1. Predict the “druggability” of a target based on its implications in a disease pathway
  2. Assess a molecule’s druggability by analyzing its ADMET properties
  3. Propose a drug intervention strategy for a particular disease and present it in professional language and ways
  4. Write a literature review as background for a drug intervention strategy or an essay on drug R&D topic
  5. Work collaboratively in a team environment
  6. Utilize concepts/principles of pharmacodynamics, pharmacokinetics and pharmaceutics in analyzing/explaining mechanisms of action of drug compounds and apply relevant techniques/methods in drug R&D

Course Content

Drug discovery overview. General strategies and concepts

Drug target discovery and lead compound discovery

Pharmacokinetics

Drug metabolism and toxicology

Prodrug design; Pharmaceutics

Lead optimization and structure-activity relationship study (pharmacodynamics)

Pharmaceutical biotechnology

Measurement of drug activity; techniques for measuring drug – target interactions

Drugs acting on various classes of drug targets

Specific topics on anticancer therapy

Assessment

Component Course ILOs tested SBS Graduate Attributes tested Weighting Team / Individual Assessment Rubrics
Continuous Assessment
Assignment 1, 3, 4, 5, 6 1. a, b, c, d
2. a, b, e, f, h
3. a, b, e, f
4. a, b, c
5. a, b, c, d, e
6. c
7. a, c
20 team See Appendix for rubric
Mid-semester Quiz
Multiple Choice Questions 1, 2, 3, 6 1. a, b, c, d
2. e, f
20 individual
Examination (2.5 hours)
Essay 1, 2, 3, 4, 6 1. a, b, c, d
2. b, e
3. f
4. a
5. c
6. c
7. a
10 individual See Appendix for rubric
Multiple Choice Questions 1, 2, 3, 6 1. a, b, c, d
2. e, f
36 individual
Short Answer Questions 1, 2, 3, 6 1. a, b, c, d
2. a, b, e
3. f
4. a
5. a, c
6. c
7. a
14 individual See Appendix for rubric
Total 100%

These are the relevant SBS Graduate Attributes.

1. Recognize the relationship and complexity between structure and function of all forms of life, resulting from an academically rigorous in-depth understanding of biological concepts

a. Possess a conceptual framework that identifies the relationships between the major domains in the field of biology.

b. Explain the relationship between structure and function of all forms of life at the molecular level

c. Explain the relationship between structure and function of all forms of life at the cellular level

d. Explain the relationship between structure and function of all forms of life at the organism level

2. Critically evaluate and analyze biological information by applying the knowledge, scientific methods and technical skills associated with the discipline

a. Identify the assumptions behind scientific problems and issues

b. Create and evaluate hypotheses

e. Analyze the validity of qualitative and quantitative scientific data

f. Evaluate results in primary biological literature

h. Identify unintended results as opportunities for discovery

3. Develop and communicate biological ideas and concepts relevant in everyday life for the benefit of society

a. Simplify and explain scientific concepts and results of experiments to a non-biologist (avoiding jargon)

b. Display and explain scientific results clearly and persuasively to peers both verbally and in writing (includes the ability to graph data appropriately and accurately).

e. Discuss current critical questions in the field of biology

f. Demonstrate an understanding of the social and natural context of knowledge (role of science in society, influence of society on science)

4. Acquire transferable and entrepreneurial skills for career development

a. Demonstrate innovative approaches to solving problems in biological science, leading to new approaches or techniques

b. Demonstrate a flair for developing new technologies, attracting funding, marketing products and respecting IP rights

c. Demonstrate a flair for conducting research

5. Develop communication, creative and critical thinking skills for life-long learning

a. Learn independently and then share that knowledge with others

b. Learn collaboratively and be willing to share expertise with peers

c. Demonstrate critical thinking skills such as analysis, discrimination, logical reasoning, prediction and transforming knowledge

d. Question the assumptions, sources, and contexts of scientific investigation

e. Demonstrate good observation skills and a curiosity about the world

6. Develop codes of social responsibility and scientific ethics, particularly in relation to biological advancement and applications

c. Respect regulations involving plagiarism and copyright

7. Demonstrate information literacy and technological fluency

a. Locate and evaluate information needed to make decisions, solve problems, design experiments, and understand scientific data

c. Evaluate and use biological databases (literature and public datasets)

Formative Feedback

The mid-term quiz and final exam have questions that address ILOs 1 to 3 and 5.
The CA component addresses ILOs 1, 3, 4, 5 and 6 as the students are required to propose a project for a novel drug intervention strategy to identify and validate a novel drug target by searching and evaluating published life science literature. This is a team-based project.

Mid-term quiz, CA project and final exam feedback given to students in different forms: classroom discussion on quiz/exam questions and project report, written feedback on exam results in NTULearn. CA project is eveluated at two stages: students first need to submit an outline of their project at mid-semester time, then their full report 3-4 weeks later.

Learning and Teaching Approach

Lectures
(24 hours)

The lectures are designed in a way that will increase your appreciation for and interest in this course module: from the study of the disease to understanding its underlining cause to how to find a therapeutic intervention to the actual design and development of a therapeutic agent.

Tutorials
(12 hours)

The course has no real separate tutorial session per se. Rather these are imbedded in the same lectures, using numerous medicinal drug examples to illustrate and enhance your understanding of the basic principles and concepts.

Reading and References

1. An introduction to medicinal chemistry, Patrick, Graham L., 5th Edition, Oxford University Press, 2013; ISBN: 9780199697397.

2.Foye's principles of medicinal chemistry, Foye, William O., 7th Edition, Lippincott Williams & Wilkins, 2012; ISBN-13: 978-1609133450.

3.Richard B Silverman, The Organic Chemistry of Drug Design and Drug Action, 2nd and 3rd Edition, Elsevier Academic Press (2014); Hardcover ISBN: 9780123820303.

4.John H Block and John M Beale, Jr, Wilson and Gisvold’s Textbook of Organic Medicinal and Pharmaceutical Chemistry, 12th Edition, 2011; ISBN: 9788184733969

5.Gary Walsh, Pharmaceutical Biotechnology: Concepts and Applications, John Wiley & Sons, Ltd, 2007; ISBN: 978-0-470-01244-4.

Course Policies and Student Responsibilities

You are expected to do all assignments by due dates and take scheduled quizzes. You are responsible to follow up with the announcements and time-table for course events.

For the team-based project assignment, every team member must contribute to the team efforts in all aspects (formulating the hypothesis, target proposal and validation, report writing and presentation, etc.) and actively participate in groups discussions.

Academic Integrity

Good academic work depends on honesty and ethical behaviour. The quality of your work as a student relies on adhering to the principles of academic integrity and to the NTU Honour Code, a set of values shared by the whole university community. Truth, Trust and Justice are at the core of NTU’s shared values.

As a student, it is important that you recognize your responsibilities in understanding and applying the principles of academic integrity in all the work you do at NTU. Not knowing what is involved in maintaining academic integrity does not excuse academic dishonesty. You need to actively equip yourself with strategies to avoid all forms of academic dishonesty, including plagiarism, academic fraud, collusion and cheating. If you are uncertain of the definitions of any of these terms, you should go to the Academic Integrity website for more information. Consult your instructor(s) if you need any clarification about the requirements of academic integrity in the course.

Course Instructors

Instructor Office Location Phone Email
Liu Chuan Fa (Assoc Prof) 03s-85 6316 2867 cfliu@ntu.edu.sg

Planned Weekly Schedule

Week Topic Course ILO Readings/ Activities
1

Drug discovery overview. General strategies and concepts

1, 2, 3, 4, 5, 6
2

Drug target discovery and lead compound discovery

1, 2, 3, 4, 5, 6
3

Pharmacokinetics (I)

1, 2, 3, 4, 5, 6
4

Pharmacokinetics (II)

1, 2, 3, 4, 5, 6
5

Drug metabolism and toxicology

1, 2, 3, 4, 5, 6
6

Prodrug design; Pharmaceutics

1, 2, 3, 4, 5, 6
7

Lead optimization and structure-activity relationship study (pharmacodynamics)

1, 2, 3, 4, 5, 6
8

Measurement of drug activity; techniques for measuring drug – target interactions

1, 2, 3, 4, 5, 6
9

Drugs acting on various classes of drug targets

1, 2, 3, 4, 5, 6
10

Pharmaceutical biotechnology (I)

1, 2, 3, 4, 5, 6
11

Pharmaceutical biotechnology (II)

1, 2, 3, 6
12

Specific topics on anticancer therapy

1, 2, 3, 6
13

Revision

1, 2, 3, 6

Appendix 1: Assessment Rubrics

Rubric for Continuous Assessment: Assignment (20%)

This is a group assignment in which your team will need to propose a druggable target for a disease/health condition of your choice. You will need to use all the knowledge you have learned from your prior courses and read, gather and analyze information from the scientific literature to propose and validate your target. You have about 2/3 of the semester to work on this assignment. You are required to submit a report and if time permits present your project.

The assignment is assessed as the following:

Collaborative team work 1.5%

Formulation of hypothesis in proposing the disease target 3.5%

Background information supporting target ID 5%

Published data supporting target validation 6%

Structure and formatting 2%

Writing and presentation 2%

Rubric for Examination: Essay (10%)

The essay will require you to synthesize, integrate, interpret/analyze course knowledge as a way to assess your overall understanding level.There will be three essay-type questions to test the understanding of student on different topics. Student is usually required to answer only two out of the three questions. Each question is scaled to about 5% of the final assessment.

This will assess the student’s ability to write (as per learning outcome #4) an essay on topics mapped to learning outcomes #1, 2, 3 and 6. A top-rated essay should show the following attributes: correct and complete understanding of the topic with, if needed, cleanly presented sketch diagrams/drawings/tables to explain difficult concept, methodology and techniques; organized and structured logically, in concise and succinct language and with clearly shown ideas and analyses.

The assessment criteria for a 10-mark exam question are shown below:

Criteria

weightage

Grade level

Excellent / outstanding

Average / good

Poor / underperform

Understanding level of the topic

5

4-5

2.5-3.5

0-2

Ability to synthesize and analyse knowledge

3

3

2

0-1

Writing

2

2

1

0

Rubric for Examination: Short Answer Questions (14%)

There are several short answer questions in the exam paper each with varying marks. The short answer questions account for about 14% of the final assessment. These short answer questions test your understanding of the basic concepts and your knowledge in the subject matter. For a 5-mark question, the rubrics are as following:

No. of marks 0-1 2-3.5 4-5
Description

Answer shows little to no understanding of the concept and low knowledge level of the subject matter.

Answer shows moderate to good understanding of the concept and moderate to good knowledge level of the subject matter.

Answer shows thorough understanding of the concept and excellent knowledge level of the subject matter.

Appendix 2: Intended Affective Outcomes

As a result of this course, it is expected you will develop the following "big picture" attributes:

Awareness of how students can use a broad range of previously acquired knowledge to solve drug-related problems

Willingness to work in a team

Willingness to set their own research agenda

Willingness to take on leadership roles

Willingness to communicate and enhance team outcomes

An ethical and honest approach to writing a project report