File(s) under permanent embargo

Reason: Under embargo until April 2022. After this date a copy can be supplied under Section 51(2) of the Australian Copyright Act 1968 by submitting a document delivery request through your library, or by emailing document.delivery@monash.edu

The development of 53BP1 inhibitors using REFiL– an efficient workflow for early stage hit to lead optimisation in FBDD

thesis
posted on 26.04.2021, 00:27 by BEATRICE CHIEW
Breast cancer is a commonly diagnosed form of cancer. A person is 6-times more likely to develop breast cancer if they have inherited mutations to the BRCA-1 gene. One potential means of preventing this is by inhibiting a protein called 53BP1. This work details the synthesis and testing of over 1000 potential drug-like compounds against 53BP1. It also demonstrates one of the first applications of a novel workflow hoped to expedite drug discovery called REFiL – the Rapid Elaboration of Fragments into Leads. In under 3 years, 7 promising leads were identified against this potential new anti-cancer target.

History

Campus location

Australia

Principal supervisor

Martin Scanlon

Additional supervisor 1

Bradley Croy Doak

Year of Award

2021

Department, School or Centre

Medicinal Chemistry

Course

Doctor of Philosophy

Degree Type

DOCTORATE