Fragment-based drug discovery for RNA targets

Kasper Plenov Lundquist, Vipul Panchal, Charlotte Held Gotfredsen, Ruth Brenk, Mads Hartvig Clausen*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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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, 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.
Original languageEnglish
Issue number17
Pages (from-to)2588-2603
Number of pages16
Publication statusPublished - 2021


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