From Target to Drug

This project aims to develop a proof-of-concept of a key enabling technology that can deliver
a step change in the speed and cost of discovering new candidate drugs. The project will
develop innovative bioinformatics technologies that can link two principal platforms of
modern drug discovery: large scale peptide screening and synthetic chemistry of small
molecule drug candidates. Large peptides libraries are already widely used to sample a vast
chemical space and identify active (binding) peptides. However, until now there has been no
cost-effective and rapid way of translating this into small molecule drug candidates other than
by using these peptides to screen large chemical libraries. This process is slow and costly and
limits the compounds that can be identified to a small, well-defined set in the chemical library,
compromising the benefits of using peptides in the first place. This process also results in
significant loss of “chemical space information” from the active peptides. This project aims to
bridge this gap and allow the outputs of large peptide screening runs to be directly and rapidly
translated into novel small molecule candidate drugs. This is now possible because of recent
advances in synthesis, handling and interrogating very large peptide screening systems.
This project is designed to demonstrate novel informatics technologies that will enable (i) A
dramatic reduction in the time (from 3 years to under 6 months) and cost (from £200M to
>£0.5M) to get from drug target to validated drug candidates. (ii) A substantial increase in the
chemical diversity of drug candidates, leading to new classes of drugs, and (iii) Strengthening
the intellectual property rights of the new chemical entities and so boosting profitability of the
industry. This project aims to slow the decline in productivity of the drug discovery industry
and enable innovative and effective medicines to be delivered to patients while minimizing
the rising costs of the NHS drug bill.