UNIVERSITY OF SARGODHA
DEPARTMENT OF CHEMISTRY
COURSE OUTLINE Fall, 2020-21
Course Title: Enzyme Kinetics and Mechanisms
Course Code: CHEM-7152
Credit Hours: 03
Instructor: DR. MUBSHARA SAADIA
Email: [email protected]
DESCRIPTION& OBJECTIVES
Aim and objectives:
The course is aimed at describing the students the biochemical reactions, nearly all of which are mediated by a series of remarkable biological catalysts known as enzymes. Enzymology, the study of enzymes, has significant importance from early days of biochemistry. From the contents, the students will get the answer of very basic and one of the central questions of biochemistry: How do enzymes work?
Following objectives will be accomplished in the course contents;
Description: The course contents are designed according to the guidelines by HEC. The study of enzymes has immense practical importance especially in some diseases;for example in inheritable geneticdisorders, there may be a deficiency or even a total absence of one or more enzymes. For other diseaseconditions, excessive activity of an enzyme may be the cause. Measurements of the activities of enzymes inblood plasma, erythrocytes, or tissue samples are important in diagnosing certain illnesses. Many drugs exerttheir biological effects through interactions with enzymes. And enzymes are important practical tools,not only in medicine but in the chemical industry, food processing, and agriculture.
The course contents will describe at beginningthe important properties of enzymes and the principles underlying their catalytic power, then the introduction of enzyme kinetics, a discipline that provides much of the framework for any discussion of enzymes. Specific examples of enzyme mechanisms are then provided and at the end with a discussion of how enzyme activity is regulated.
Learning Outcome: The contents are aimed to develop understanding of the students about the basic and mathematical aspects of enzyme kinetics, enzyme catalysis, and enzyme inhibition and regulation.Kinetic data, combined with detailed information about an enzyme’s structure and its catalytic mechanisms, provide some of the most powerful clues to the enzyme’s biological function and may suggest ways to modify it for therapeutic purposes.
READINGS
CONTENTS
Fundamentals of enzyme kinetics, Kinetics includes steady state, stopped-flow, single and multi-substrate kinetics; Derivation of rate equations; Applications of Michaelis-Menton equation; use of lineweaver-Burk plot and Eddie Hofstee plot for determination of Vmax and km; Free energy of activation and effects of enzymes; Mechanisms of enzyme catalyzed reactions; Allosteric control and regulation of enzymes; effects of pH, temperature and inhibitors; Kinetics of competitive, Non-Competitive and mixed inhibition; Kinetics of displacement reactions, ordered and random double displacement reactions.
COURSE SCHEDULE
Week |
Topics and Readings |
Dates
|
1. |
Lecture 1. Fundamentals of enzyme kinetics; Introduction: General properties of enzymes (Reading No.2; page 323) enzyme classification (Reading No.1; pages 191-193) |
28-10-2020 |
Lecture 2. How Enzymes Work (Reading No.1; pages193-197) |
29 |
|
2. |
Lecture 3. How Enzymes Work(Reading No.1; pages193-197) |
04-11-2020 |
Lecture 4. Binding Energy Contributes to Reaction Specificity and Catalysis (Reading No.1; pages 198-200) |
05 |
|
3. |
Lecture 5. Catalytic Mechanisms (Reading No.2; pages 330-339) |
11 |
Lecture 6. Catalytic Mechanisms (Reading No.2; pages 330-339) |
12 |
|
4. |
Lecture 7. Enzyme Kinetics as an Approach to Understanding Mechanism: Derivation of rate equations; Applications of Michaelis-Menton equation;(Reading No.1; pages 202-203) |
18 |
Lecture 8. Use of lineweaver-Burk plot (Reading No.1; pages 204-206) |
19 |
|
5. |
Lecture 9. Single and multi-substrate kinetics: Many Enzymes Catalyze Reactions with Two or More Substrates(Reading No.1; pages 207-208) |
25 |
Lecture 10. Kinetics of displacement reactions, ordered and random double displacement reactions. (Reading No.2; pages 375-376) |
26 |
|
6. |
Lecture 11. Mechanisms of enzyme catalyzed reactions: The Thymotrypsin Mechanism (Reading No.1; pages 213-218) |
02-12-2020 |
Lecture 12. The Hexokinase and Enolase mechanisms (Reading No.1; pages 218-221) |
03 |
|
7. |
Lecture 13. Lysozyme mechanism (Reading No.1; pages 222-225) |
09
|
Lecture 14. Allosteric control and regulation of enzymes: Allosteric Enzymes (Reading No.1; pages 225-230) |
10 |
|
8. |
Lecture 15. Allosteric Enzymes (Reading No.1; pages 225-230) Lecture 16. Effects of pH, temperature and inhibitors: Enzymes Are Subject to Reversible or Irreversible Inhibition (Reading No.1; pages 209-212) |
16 |
17 |
||
9. |
Lecture 17. Enzymes Are Subject to Reversible or Irreversible Inhibition (Reading No.1; pages 209-212) |
23 |
Lecture 18. Enzyme Activity Depends on pH (Reading No.1; pages 212-213) |
24 |
|
10. |
Mid-term Examination |
December 25, 2020 to January 10, 2021) |
11. |
Lecture 19. Drug Designing (Reading No.2; Pages 394-400) |
13-01-2021 |
Lecture 20. Drug Designing (Reading No.2; Pages 394-400) |
14 |
|
12. |
Lecture 21. Drug Designing (Reading No.2; Pages 394-400) |
20 |
Lecture 22. Drug Designing (Reading No.2; Pages 394-400) |
21 |
|
13. |
Lecture 23. Practical determination of Vmax an KM: (Reading No.1; Problem No. 19 Working with Kinetics, Page 237) |
27 |
Lecture 24. Exercise: Some problem solutions (Reference: Reading No.2, Page 401-402) |
28 |
|
14. |
Lecture 25. Exercise: Some problem solutions (Reference: Reading No.2, Page 401-402) |
03-02-2021 |
Lecture 26. Assignment 1: Clinical Application of Differential Enzyme Inhibition (Reference: Reading No.1, Page 247) |
04 |
|
14. |
Lecture 27. Assignment 2: Observing Enzyme Action by X-Ray Crystallography (Reference: Reading No.2; box 11-2, page 342) |
10 |
Lecture 28. Assignment 3: Evidence for Enzyme–Transition State Complementarity (Reference: Reading 1, BOX 6–3, page 220)
|
11 |
|
15. |
Lecture 29. Assignment 4-5: Enzyme Inhibitors and Rational Drug Design 1. Dihydrofolate Reductase (Reference: prerequisite Chapter 12 of reading No. 2), HIV Enzyme Inhibitors (Reference: Reading No. 2, BOX 12-4, pages 384-385) |
17 |
Lecture30. Assignment 6-7: Case study 13, Inhibition of Alcohol Dehydrogenase (Reference: prerequisite Chapter 12 of reading No. 2), Inhibition of Carbonic Anhydrase by Acetazolamide (Reference: Reading No.1page 247) |
18 |
|
16. |
Presentations |
24,25-02-2021 |
17 |
Final Term Examination (1st semester) |
March 01 to 05, 2021 (Monday to Friday) |
RESEARCH PROJECT
No research project is assigned.
ASSESSMENT CRITERIA
Sessional marks (Presentation+Participation) = 20
Project: 0
Presentation: 12
Participation: 08
Final Marks: Mid+Final+Sessional (30+50+20) = 100
RULES AND REGULATIONS
Minimum 80% class attendance is required.