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Fragment-based drug discovery supports drugging 'undruggable' protein-protein interactions.
- Source :
-
Trends in biochemical sciences [Trends Biochem Sci] 2023 Jun; Vol. 48 (6), pp. 539-552. Date of Electronic Publication: 2023 Feb 24. - Publication Year :
- 2023
-
Abstract
- Protein-protein interactions (PPIs) have important roles in various cellular processes, but are commonly described as 'undruggable' therapeutic targets due to their large, flat, featureless interfaces. Fragment-based drug discovery (FBDD) has achieved great success in modulating PPIs, with more than ten compounds in clinical trials. Here, we highlight the progress of FBDD in modulating PPIs for therapeutic development. Targeting hot spots that have essential roles in both fragment binding and PPIs provides a shortcut for the development of PPI modulators via FBDD. We highlight successful cases of cracking the 'undruggable' problems of PPIs using fragment-based approaches. We also introduce new technologies and future trends. Thus, we hope that this review will provide useful guidance for drug discovery targeting PPIs.<br />Competing Interests: Declaration of interests None declared by authors.<br /> (Copyright © 2023 Elsevier Ltd. All rights reserved.)
- Subjects :
- Protein Binding
Drug Discovery
Subjects
Details
- Language :
- English
- ISSN :
- 0968-0004
- Volume :
- 48
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Trends in biochemical sciences
- Publication Type :
- Academic Journal
- Accession number :
- 36841635
- Full Text :
- https://doi.org/10.1016/j.tibs.2023.01.008