CENTRE FOR THERAPEUTICS DISCOVERY

Drug Targets

MRC funds high quality research in all areas of biomedical science, and thus selected drug targets cover a diverse range of therapeutic areas including:

• Infectious Diseases
• Neurological Disorders
• Oncology
• Cardiovascular Disease
• Mental Health
• Reproductive Health
• Diabetes & Metabolic Disease
• Diseases of the Elderly
• Vision & Hearing
• Arthritis & Rheumatism
• Respiratory Disease
• Oral Health

MRCT is well positioned to identify potential novel drug targets and actively seeks new projects from the MRC science base. In addition, there is basic research underway which is not tied to one particular area and could lead to the discovery of common underlying mechanisms.

The MRCT CTD works closely with the MRCT Intellectual Property Division and is rigorous in the selection of well-defined and characterised targets, and considers novelty, validation and ‘druggability’ (see section describing Criteria for Selection of Drug Targets). In addition, the group works on targets where there is a clear strategy for progression and development and where there is complementary scientific expertise available within the MRC. MRCT are also diligent with respect to obtaining patent protection for targets, assays and novel chemical scaffolds for medicinal use.

Activities

The specific activities of the CTD include

• development and optimisation of simple, robust and inexpensive assays suitable for high-through put screening
• screening of a library containing a diverse set of up to 100,000 small drug-like compounds and the identification of novel ‘hit’ compounds
• evaluation and profiling of ‘hit’ compounds for specific and genuine activity against the target and assessment of their potential to be developed into drugs
• progression of ‘hit’ compounds with desirable properties into ‘Hit–to-Lead’ medicinal chemistry in order to improve potency and selectivity and develop desirable ADMET characteristics
• evaluation of potent and selective lead molecules for efficacy in cellular, as well as animal models of disease and detailed studies on their mechanism of action
• Management of associated intellectual property and identification of suitable partners for licensing and further drug development

The activities of MRCT CTD are complemented by the knowledge and strengths available within the MRC science base, particularly in the areas of target validation and mechanism of action of identified lead compounds. Where possible, MRC expertise in structural biology is used in CTD programmes.