Chemical Biology: Approaches to Drug Discovery and Development to Targeting Disease

Chapter 1: The Role of Chemical Biology in Drug Discovery

Andrew J. Pope

Platform Technology & Science, GlaxoSmithKline, Collegeville, Pennsylvania

Chemical biology methods are central to the discovery of new medicines. The development of new approaches and techniques has accompanied, and been central to, major advances in understanding of disease biology and a move from pharmacology-driven to molecular-medicine-based drug discovery. This chapter will highlight some critical contributions from chemical biology methods in the context of a high-level overview of drug discovery as practiced currently.

1.1 Introduction

The discovery and development of new medicines is a highly complex, time-consuming, and expensive endeavor that has faced many changes and challenges over the last two decades [1]. On the one hand, the pace of scientific discovery within the biomedical sciences has proceeded at unprecedented levels, fueled by dramatic advances in technology (e.g., Genomics [2] and High Throughput Screening [3, 4]). On the other hand, the development of new medicines has never been more challenging in terms of cost, time, and the regulatory environment [5–8]. However, it is inevitable that societies will strive continually to improve their economic circumstances and improve human health and that discovery and access to medicines will play a critical role. The development and application of chemical biology methods are central to many aspects of the pursuit of medicines and are providing ...