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Printable Handouts
Navigable Slide Index
- Introduction
- Goals
- Key references and disclaimer
- Enzymes as drug targets
- Drug discovery and mechanistic biochemistry
- Why are enzymes such good drug targets?
- Methotrexate is an inhibitor of DHFR
- DHFR interactions with methotrexate and DHF
- Other reasons to study enzymes
- Protein-ligand binding at equilibrium
- Receptor-ligand binding at equilibrium
- Reversible forces in enzyme-ligand binding
- Mass conservation equations
- Ligand titration curves
- Applications of the Langmuir isotherm equation
- Competitive ligand binding to a common target
- Enzyme reaction mechanisms
- Defining features of enzyme catalysis
- Simple enzyme reactions
- Transition state reaction
- Transition state theory in enzymology (1)
- Transition state theory in enzymology (2)
- Characteristics of enzyme active sites
- Active site structure and substrate specificity
- Thermodynamic cycle for substrate transition
- Enzymes enhance the rates of chemical reactions
- Transition state theory in enzymology (3)
- Transition state theory in enzymology (4)
- Laboratory measures of enzyme reactions
- Velocity of enzyme-catalyzed reactions
- Henri-Michaelis-Menten rapid equilibrium model
- Definition of steady state
- Briggs and Haldane steady state model (1)
- Briggs and Haldane steady state model (2)
- Substrate titration during steady state (1)
- Substrate titration during steady state (2)
- Effect of pH on steady state kinetic parameters
- Free energy relationships for kinetic constants
- Bisubstrate reactions
- Random ternary complex mechanism
- Compulsory ordered ternary complex mechanism
- Double displacement (ping-pong) mechanism
Topics Covered
- Enzymes as targets for drug discovery
- Protein-ligand binding equilibria
- Enzyme reaction mechanisms
- Structure and function of enzyme active sites
- Measuring enzyme velocity in the laboratory
- Reversible modes of enzyme inhibition
- Enzyme inhibition as a mechanism of pharmacological intervention in disease
- Clinical value of different inhibition modalities
- Non-classical inhibition
- Enzyme assays and screening criteria
- Lead optimization
- Summary: basic information to look for
Talk Citation
Copeland, R. (2013, September 23). Enzymology in drug discovery 1 [Video file]. In The Biomedical & Life Sciences Collection, Henry Stewart Talks. Retrieved December 5, 2024, from https://doi.org/10.69645/HKPU7536.Export Citation (RIS)
Publication History
Financial Disclosures
- Prof. Robert Copeland has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.
Enzymology in drug discovery 1
Published on September 23, 2013
42 min
A selection of talks on Biochemistry
Transcript
Please wait while the transcript is being prepared...
0:00
Hello and welcome to a series of lectures on entomology and drug discovery.
My name is Robert Copeland and I will guide you through this series of two lectures.
In the first lecture,
we'll talk about the fundamental properties of enzymes,
catalysis and what makes these enzymes attractive targets for drug discovery.
In the second lecture,
we'll talk about the interactions of small molecule reversible inhibitors with
enzyme targets that form the basis of much of the pharmacology of small molecule drugs.
0:41
The goals of this series of two lectures or to answer the following questions.
What opportunities for Inhibitor interactions exist with an enzyme target?
How did these arise from consideration of the reaction mechanism?
That will be in large part covered in lecture one.
How inhibitors properly evaluated in terms of potency,
selectivity and mode of action important
questions for the medicinal chemist which will be covered in lecture two,
and what information should medicinal chemists and pharmacologists expect from
their biology and biochemistry colleagues
that will be covered across both of the lectures.
1:24
The materials to be covered in this series of two lectures are
drawn largely from copyrighted material sources.
For the most part, the materials covered come from
two books both of which were authored by myself.
The first book is entitled Enzymes,
A Practical Introduction to Structure Mechanism and Data Analysis,
second edition, published in 2000 by John Wiley and Sons.
The second book is Evaluation of Enzyme Inhibitors In Drug Discovery.
A guide for medicinal chemists and pharmacologists also published by Wiley in 2005.
Both of these books make very good supplements
to the lecture materials that we will be covering,
and anyone interested in obtaining these books can do so
directly from John Wiley or from any major bookseller.