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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

People

ORCID iD

Robert Troup (Student)

Publications

10 25 50

Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/R513325/1 30/09/2018 29/09/2023
2106286 Studentship EP/R513325/1 30/09/2018 30/03/2022 Robert Troup