Research Groups

Drug Discovery

The burgeoning burden of disease on the one hand and the huge market for leading therapeutic drugs of over $350 billion per year on the other is driving the pursuit of new methods in synthesis and drug development and drug target identification. The need for safe, effec tive medicines must take into account the fierce competition in the drug-development industry which is experiencing considerable cost pressures. A traditional drug-discovery approach is to identify a therapeutic target, link this to a specific biological mechanism, and thereby provide a focus for a discovery effort. Identification of effective or lead compounds has benefited from the advent of high-throughput screening methods that enable a large number of compounds to be screened in a relatively short time. Recent advances in the methodology of synthetic chemistry have facilitated the rapid construction of lead analogs. These lead compounds can then be subjected to a variety of substrate binding and toxicological tests to determine their efficacy as drugs.

During 2008 the Drug Discovery Signature Theme has made significant progress towards identifying new and strengthening existent research projects. These are all linked to three technological platforms which form an essential basis for these projects, namely Synthesis of small molecules in drug development, Structural biology of proteins and protein-ligand complexes and Expression and purification of proteins. Professor Roger Hunter of the Department of Chemistry is the Director of the Signature Theme.

A joint venture between UCT, AngioDesign Inc and the Cape Biotech Trust has resulted in the incorporation of AD Therapeutics (Pty) Ltd. The core business of this venture is the structure-based design, development and commercialisation of next-generation drugs for validated disease targets. The ACE inhibitor work has formed the cornerstone of this new company. Ace is a drug-target for hypertension. This demonstrates the potential of the Signature Theme to develop spin-out companies.

Significant progress has been made by Signature Theme member Professor Kelly Chibale, who holds an NRF Research Chair in Drug Discovery, towards the establishment of a drug discovery centre at UCT focusing on integrating drug metabolism and pharmacokinetic studies into drug-discovery as it relates to hits to leads and lead optimisation medicinal chemistry. The Medicines for Malaria Venture, Cape Biotech Trust and key pharmaceutical companies such as Pfizer have already committed their support. The centre will be hosted in the Department of Chemistry and will be the first facility of its type in Africa.