Chemical Synthesis and Biological evaluation of improved PROTACS based on a novel Design Strategy

Lead Research Organisation: University of Southampton
Department Name: Sch of Chemistry

Abstract

The project concerns a novel approach to optimise the activity and physical properties of a relatively new class of bioactive compounds, PROTACs, which are of huge current interest to achieve targeted protein degradation. The organic chemistry aspect consists of the chemical synthesis of a series of fluorinated precursors followed by incorporation into PROTACs. The medicinal chemistry aspect consists of the evaluation of the synthesised PROTACs against a panel of medically relevant proteins while on placement at our industrial collaborator, AstraZeneca. The project originates from the world-leading expertise in organofluorine medicinal chemistry. While synthetic organic chemistry is a key aspect of the project, it contains a strong medicinal chemistry element, and you will become familiar with the significant role of fluorination in current drug optimisation While synthetic organic chemistry is a key aspect of the project, it contains a strong medicinal chemistry element, and you will become familiar with the significant role of fluorination in current drug optimisation and with the burgeoning field of PROTACs

Publications

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Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/R513325/1 01/10/2018 30/09/2023
2106286 Studentship EP/R513325/1 01/10/2018 31/03/2022 Robert Troup