Chem 162 Main Page

Chem 162/262

Drug Design

Lecturer:

Dr. Kalju Kahn
Office: PSB-N 1511
Office hours: Tue and Fri (12:00-1:00 PM) or by appointment
Phone: 893-6157
E-mail: kalju@chem.ucsb.edu
Website: http;//www.chem.ucsb.edu

Teaching Assistant

August Estabrook
Office hours: Chem 1148, 
Phone: 893-8283 
E-mail: aestabrook@chem.ucsb.edu

Mission statement

To teach principles that govern the process of modern drug discovery and development. Students in the course follow a path similar to that taken by real-life drug developers by learning important elements of the drug design process in a logical order.

Schedule

      Lecture:        MWF 10:00-10:50   Place:	Webb 1100  
      Computer Lab:   Open access		Place:  Chem 1153

Syllabus	General information about the course.	PDF
Textbook	The Organic Chemistry of Drug Design and Drug Action by Richard B. Silverman (Second Edition)	$80 (Amazon)
Sample Lecture	Target Validation. (No Password Needed) Warning: Large File	PDF WAV
Year 2003	Drug Desing (by Dr. Norbert Reich) website for Spring 2003	Link
Upload	Submit your assignments as MS Word or PDF files	Link
Exam	Exam Preparation Guide	PDF
Exam	Sample questions from my last year Chem 112L test	PDF
Exam Key	Sample answers to some questions in the exam	PDF

Lecture Notes

Course notes will be posted here before 7:30 a.m. of the lecture day. These files are password-protected. Contact your instructor to obtain the password.

Notes	Powerpoint Lecture Note Pages in PDF	Acrobat
March 29	Overview of the course. History of drug design	PDF
March 31	Current trends and future of drug design. Diseases	PDF
April 2	Target Validation	PDF
April 5	Target Validation	PDF
April 7	Enzymes and Receptors	PDF
April 9	Receptors, Lead Identification, Interactions	PDF
April 12	Lead Modifications	PDF
April 14	Pharmacokinetics	PDF
April 16	Enzyme Mechanisms	PDF
April 19	Enzyme Kinetics	PDF
April 21	Enzyme Inhibition	PDF
April 23	Enzyme Inactivation; Receptor Studies	PDF
April 26	Displacement Assay; Structure-Based Drug Design	PDF
April 28	Structure-Based Drug Design: Principles	PDF
April 30	Structure-Based Drug Design: Docking and Visualization	PDF
May 3	Structure-Based Drug Design: Free Energy Simulations	PDF
May 5	Combinatorial Chemistry	PDF
May 10	QSAR	PDF
May 12	Drug Metabolism	PDF
May 14	Drug Metabolism	PDF
May 17	Prodrugs and Drug Delivery	PDF
May 19	Pharmacogenomics	PDF
May 21	Pharmacogenomics	PDF
May 24	Nucleic Acid Drugs	PDF
June 2	Pharmaceutical Industry: Jobs, Trends, and Outlook	PDF

Required Literature

Literature	Required reading in PDF	Acrobat
General	From Serendipity to Rational Drug Design	PDF
History	Drug Discovery: A Historical Perspective	PDF
Future	Drug Research: Myths, Hype and Reality	PDF
Future	Cell-based uHTS Chemical Genomic Drug Discovery	PDF
Validation	Drug Discovery in the Post-Genomic Era	PDF
Validation	DNA Microarrays	PDF
Validation	mRNA Knockdown: Antisense, Ribozymes, RNAi	PDF
Validation	Proteomics: Proteins Rule	PDF
Validation	Single Nucleotide Polymorphisms: Review	PDF
Targets	Protein Kinases	PDF
Leads	HIV Protease Inhibitors	PDF
ADME	Predicting Pharmacokinetics	PDF
Enzymes	Transition State Binding	PDF
SBDD	The Process of Structure-Based Drug Design	PDF
SBDD	High-throughput docking	PDF
SBDD	Nicotinic Acetylcholine Receptor: Docking	PDF
Pharmacogenomics	Better Therapeutics through Microarrays	PDF
Gene Therapy	X-Linked SCID: Gene Therapy and Leukemia	PDF
Antisense Therapy	Novel Antisense and PNA Strategies	PDF
Protein Therapy	Preclinical safety of Biopharmaceuticals	PDF
Protein Therapy	Glycoengineering	PDF

Suggested Literature

Assignments

The assignments are posted one week before the due date. Answers shall be submitted electronically no later than the midnight of the due date.

Assignments		Acrobat
0	Drug Design Proposal Tips.	PDF
1	Target Validation	PDF
2	Biomolecular Interactions. Pharmacokinetics. Receptors and Enzymes.	PDF
2	Question 2C Inhibitor Structure.
3	Enzyme Mechanisms.	PDF
4	Enzyme Inhibition and Inactivation.	PDF
5	Structure-Based Drug Design.	PDF
6	QSAR.	PDF
7	Drug Metabolism and Prodrugs.	PDF
8	Gene Therpay, Protein Drugs, Intellectual Property.	PDF

Answer Keys

The assignment keys are typically posted one week after the due date.

Keys		Acrobat
1	Target Validation	PDF
2	Biomolecular Interactions. Pharmacokinetics. Receptors and Enzymes.	PDF
3	Enzyme Mechanisms.	PDF
4	Enzyme Inhibition and Inactivation.	PDF
5	Structure-Based Drug Design.	PDF
6	QSAR.	PDF
7	Drug Metabolism and Prodrugs.	PDF
8	Gene Therpay, Protein Drugs, Intellectual Property.	PDF

Glossary

Students in this course encounter many terms which have specific meaning in the context of drug design and medicine. You may find our glossary helpful when reading some of the assigned papers. If you encounter a term that is not in this dictionary, you could try a specialized medicinal chemistry glossary at www.chem.qmw.ac.uk/iupac/medchem ,an on-line dictionary at www.dictionary.com or an on-line encyclopedia at www.wikipedia.com . Feel free to send any additions and suggestions to Kalju Kahn

Chem 162/262 Drug Design