Platform development to improve valuable drug optimisation

GSK
University of Strathclyde

A lack of defined binding sites on proteins of interest often causes issues within the traditional drug discovery process, as potential drug targets are not as easy to control. The result of this is “undruggable” targets, causing obvious barriers within the drug discovery pathway.

Proteolysis Targeting Chimeras (PROTACs) are a rapidly evolving new type of drug, currently sparking great excitement within the pharmaceutical and biotechnology industries. PROTACs offer a unique opportunity to target these ‘undruggable’ biological targets. While the traditional aim within drug discovery has been to inhibit a protein’s function using small molecule drugs that bind to target sites, PROTACs exploit the body’s own mechanisms to tag and degrade desired proteins of interest altogether. However, PROTACs are typically double the size and complexity of normal drugs, so their synthesis is far from simple.

Rebecca’s project aims to tackle this challenge through the development of a multistep platform capable of producing hundreds of PROTACs simultaneously. The methods developed in the project will offer new capabilities for efficient and sustainable production of PROTACs, increase the pace of data generation, and accelerate the exploration of structure-activity relationships. 

Biography

Prior to her PhD, Rebecca received a First-class Masters in Chemistry from the University of Bristol, during which she completed a placement year within drug discovery at Evotec and received three ‘EVOawards’ for her excellent contributions to the project team. Since starting her PhD Rebecca has obtained significant results, which has enabled her to present at many symposia, including the EFMC Young Medicinal Chemists’ Symposium where she was awarded one of the three conference poster prizes.