Lamoree, Bas orcid.org/0000-0001-6410-5950 and Hubbard, Roderick Eliot orcid.org/0000-0002-8233-7461 (2017) Current perspectives in fragment based lead discovery (FBLD). Essays in Biochemistry. pp. 453-464. ISSN 1744-1358
Abstract
It is over 20 years since the first fragment-based discovery projects were disclosed. The methods are now mature for most ‘conventional’ targets in drug discovery such as enzymes (kinases and proteases) but there has also been growing success on more challenging targets, such as disruption of protein–protein interactions. The main application is to identify tractable chemical startpoints that non-covalently modulate the activity of a biological molecule. In this essay, we overview current practice in the methods and discuss how they have had an impact in lead discovery – generating a large number of fragment-derived compounds that are in clinical trials and two medicines treating patients. In addition, we discuss some of the more recent applications of the methods in chemical biology – providing chemical tools to investigate biological molecules, mechanisms and systems.
Metadata
Item Type: | Article |
---|---|
Authors/Creators: |
|
Copyright, Publisher and Additional Information: | © 2017 The Author(s). |
Dates: |
|
Institution: | The University of York |
Academic Units: | The University of York > Faculty of Sciences (York) > Chemistry (York) |
Depositing User: | Pure (York) |
Date Deposited: | 09 Nov 2017 14:20 |
Last Modified: | 19 Feb 2025 17:20 |
Published Version: | https://doi.org/10.1042/EBC20170028 |
Status: | Published |
Refereed: | Yes |
Identification Number: | 10.1042/EBC20170028 |
Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:123830 |
Download
Filename: 453.full.pdf
Description: Current perspectives in fragment-based lead discovery (FBLD)
Licence: CC-BY-NC-ND 2.5