Dynamic Chemical Probes with New Modes of Action to Deconvolute Therapeutic Protein-Protein Interaction Networks
Lead Research Organisation:
University of Southampton
Department Name: Sch of Chemistry
Abstract
This project will develop a strategy for the development and evaluation of a 'toolkit' of covalent chemical probes for the inhibition of therapeutically-relevant protein-protein interactions (PPIs) that are critical in myriad diseases. These agents will consist of conformationally-preorganised alpha helical peptidomimetic scaffolds armed with electrophilic warheads. The scaffolds may be functionalised to provide complementary contacts for a given protein surface and to form a covalent bond between the mimetic and a nucleophilic amino acid side-chains (N- and O-centred) displayed on the surface of the target protein. The agents will be designed to bind via either a dynamic or irreversible mechanism with the potential for a high-affinity interaction. Their utility as a general method for mediating PPIs will be evaluated against therapeutically important targets using proteomic workflows in collaboration with Drs Rob Ewing and Paul Skipp.
Organisations
Studentship Projects
Project Reference | Relationship | Related To | Start | End | Student Name |
---|---|---|---|---|---|
EP/R513325/1 | 01/10/2018 | 30/09/2023 | |||
2284163 | Studentship | EP/R513325/1 | 01/10/2019 | 31/03/2023 | Rose Banniser |