Fragment-Based Drug Discovery for RNA Targets |
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Authors: | Kasper P. Lundquist Dr. Vipul Panchal Prof. Charlotte H. Gotfredsen Prof. Ruth Brenk Prof. Mads H. Clausen |
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Affiliation: | 1. Center for Nanomedicine and Theranostics, Department of Chemistry, Technical University of Denmark, Kemitorvet 207, 2800 Kgs. Lyngby, Denmark;2. Department of Biomedicine, University of Bergen, Jonas Lies vei 91, 5020 Bergen, Norway;3. NMR Center ⋅ DTU, Department of Chemistry, Technical University of Denmark, Kemitorvet 207, 2800 Kgs. Lyngby, Denmark |
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Abstract: | 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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Keywords: | drug discovery fragments RNA screening |
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