Journal
CHEMMEDCHEM
Volume 16, Issue 17, Pages 2588-2603Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202100324
Keywords
drug discovery; fragments; RNA; screening
Categories
Funding
- Novo Nordisk Foundation [NNF19OC0055818]
- Carlsberg Foundation [CF19-0072, CF17-0795]
- DTU
- Ministry of Higher Education and Science [5072-00019B]
- Villum Foundation [00007303]
- Technion
- Research Council of Norway
- Joint Programming Initiative on Antimicrobial Resistance, JPIAMR (Explore) [297192, 261961, 294594]
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The rapid development in fragment-based drug discovery and medicinal targeting of RNA has opened up possibilities for combining technologies and methods in novel ways. This review discusses the use of fragment-based screening against RNA targets, including the latest screening and hit validation methods, and provides insights on future perspectives in this field.
Rapid development within the fields of both fragment-based drug discovery (FBDD) and medicinal targeting of RNA provides possibilities for combining technologies and methods in novel ways. This review provides an overview of fragment-based screening (FBS) against RNA targets, including a discussion of the most recently used screening and hit validation methods such as NMR spectroscopy, X-ray crystallography, and virtual screening methods. A discussion of fragment library design based on research from small-molecule RNA binders provides an overview on both the currently limited guidelines within RNA-targeting fragment library design, and future possibilities. Finally, future perspectives are provided on screening and hit validation methods not yet used in combination with both fragment screening and RNA targets.
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