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Fragment‐Based Drug Discovery for RNA Targets
Author(s) -
Lundquist Kasper P.,
Panchal Vipul,
Gotfredsen Charlotte H.,
Brenk Ruth,
Clausen Mads H.
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100324
Subject(s) - fragment (logic) , virtual screening , computational biology , drug discovery , rna , small molecule , computer science , chemistry , biology , bioinformatics , biochemistry , algorithm , gene
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.