Download CHEM 352-BIO 352-Introduction to Drug Discovery

Lahore University of Management Sciences
Introduction to Drug Discovery & Development
Course code: Chem-352/Bio-352
Semester offered: Fall 2012-13
Instructors
Room No.
Office Hours
Email
Telephone
Secretary/TA
TA Office Hours
Course URL (if any)
Dr. Rahman S. Z. Saleem (lead; SSE-Chemistry)
Dr. Kamran Haider (SSE-Biology)
Dr. Sohail A. Qureshi (SSE-Biology)
9-513
TBA
[email protected]
8215
Course Basics
Credit Hours
Lecture(s)
Recitation (per week)
Lab (if any ) per week
Tutorial (per week)
Course Distribution
Core
Elective
Open for Student Category
Closed for Student Category
3
Nbr of Lec(s) Per Week
Nbr of Rec (s) Per
Week
Nbr of Session(s) Per
Week
Nbr of Tut(s) Per
Week
2
0
Duration
Duration
0
Duration
0
Duration
75 minutes each
X
COURSE DESCRIPTION
Introduction of Drug Discovery and Development is designed for students majoring in Biology or Chemistry (or outside clinicians or
pharmacologists) who are keen to learn about how drugs against a bevy of diseases are developed using modern biological and medicinal
chemistry methods. Initial phase of this course is devoted to understanding the underlying causes of disease and the process through which
disease causing molecules are identified. Subsequent series of lectures cover how cell-based and in vitro biochemical assays are developed and
screened, and how lead compounds are identified, optimized and readied for clinical trials. Due to its wide-spread use and success, particular
emphasis is placed on structure-based (or rational) drug design using 3-D in silico modeling of targeted molecule. Drug metabolism, delivery and
formulation also receive coverage in separate sessions. Final phase of this course deals with economics of drug development as well as legal and
ethical issues that are associated with clinical trials and marketing of drugs.
COURSE PREREQUISITE(S)
CHEM-101 and BIO-101
COURSE OBJECTIVES
Lahore University of Management Sciences
The overarching objective of this course is to introduce students to the process of how drugs are developed for use in humans or
animals.
Learning Outcomes
After taking this course students should have a basic understanding of:

Molecular basis of disease and how biological molecules are identified and targeted for drug development

How biological assays are developed, screened and lead compounds identified

Structure based drug design and development using in silico modeling
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Chemical basis of drug design
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Process of taking lead compounds into clinical trials and subsequent approval by drug agencies
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Economic and legal aspects of drug development

Drug development in the Pakistani context
Grading Breakup and Policy
Assignment(s): 20%
Midterm exam: 40%
Final exam: 40%
Examination Detail
Midterm
Exam
Yes/No: Yes
Combine/Separate: Combine
Duration: 2 hours
Preferred Date: During class time
Exam Specifications: Closed book; no notes or calculator
Final Exam
Yes/No: Yes
Combine/Separate: Combine
Duration: 3 hours
Exam Specifications: Closed book; no notes or calculator
Lahore University of Management Sciences
COURSE CONTENT
Lecture
Topics
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Introduction
Drug Discovery – A Historical Perspective
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Drug Development in the 21 Century
Identification of Drug Targets
Assay Development
Drugability of Target Molecules
Potential Sources of Drugs
Compound Libraries: Synthesis, Storage and Use
Lead Compound Identification by HTS
Stereochemistry in Drug Development
Use of Proteins, Nucleic Acids and Antibodies as Drugs
Structure-Based Drug Design
Introduction to Molecular Visualization and Modeling
HANDS-ON SESSION-1
Virtual Screening and High-Throughput Molecular
Docking
Enhancing Lead Compound Efficiency via StructureActivity Relationship (SAR)
Advanced Computational Methods for Ligand
Optimization
HANDS-ON SESSION-2
Pharmacodynamics, - kinetics and -genomics
Drug Delivery and Routes of Administration;
Formulation of Drugs
Nanoparticles in Drug Delivery
Animal Models and Clinical Trials
New Drug Approval & Large-Scale Manufacturing
Drugonomics
Legal Issues, Biosimilars and Generics
Ethics of Drug Discovery & Marketing
Low Hanging Fruits No More!
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21 Century R&D in Pharmaceutical Industry
Pharmaceutical Industry in Pakistan
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Recommended
Readings
Objectives/
Application
Textbook(s)/Supplementary Readings
The course covers a wide spectrum of topics that are not available in a single book. However, following books can be consulted:
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1. Wilson & Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry; John Block, John M. Beale, 12 edition, Lippincott
Williams & Wilkins, A Wolters Kluwer Business 2011.
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2. The organic chemistry of drug design and drug action, Richard B. Silverman, 2 edition, Elsevier Academic Press, 2004
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3. Text book of drug design and discovery, Povl Krogsgaard-Larsen, Ulf Madsen, Kristian Stromgaard, 4 edition, CRC Press 2009
4. Computational drug design: A Guide for Computational and Medicinal Chemists; David C. Young, John Wiley & Sons, Inc. 2009
5. Structural Bioinformatics; Philip E. Bourne and Helge Weissig; John Wiley & Sons, Inc. 2009.