The design, synthesis and application of covalent fragment libraries

Lead Research Organisation: Newcastle University
Department Name: Sch of Natural Sciences & Env Sciences

Abstract

"Covalent drugs have undergone a renaissance recently, partly due to the success of cancer treatments such as ibrutinib and osimertinib. Covalent inhibitors can have improved efficacy and specificity. However, new methods for their discovery are highly desirable.

Fragments are an effective approach to new candidate drugs and are of great interest in covalent drug discovery.

The project will explore new fragment-based approaches to covalent inhibitors by synthesising probe compounds to define the ideal properties of covalent fragment leads, build a covalent library and incorporate these fragments into a larger DNA-encoded library.

The compounds will be tested in representative protein targets."

Publications

10 25 50

Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/S022791/1 30/04/2019 30/10/2027
2599238 Studentship EP/S022791/1 30/09/2021 29/09/2025 Holly Walker