Enzymology in drug discovery 1

Published on September 23, 2013   42 min

Other Talks in the Series: Small Molecule Drug Discovery

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.
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.
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.