Fragment-Based Approaches to Identify RNA Binders

Suresh Blessy M.; Taghavi Amirhossein; Childs-Disney Jessica L.Disney Matthew D.

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Fragment-Based Approaches to Identify RNA Binders

机译：Fragment-Based Approaches to Identify RNA Binders

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Although fragment-based drug discovery (FBDD) has beensuccessfullyimplemented and well-explored for protein targets, its feasibilityfor RNA targets is emerging. Despite the challenges associated withthe selective targeting of RNA, efforts to integrate known methodsof RNA binder discovery with fragment-based approaches have been fruitful,as a few bioactive ligands have been identified. Here, we review variousfragment-based approaches implemented for RNA targets and provideinsights into experimental design and outcomes to guide future workin the area. Indeed, investigations surrounding the molecular recognitionof RNA by fragments address rather important questions such as thelimits of molecular weight that confer selective binding and the physicochemicalproperties favorable for RNA binding and bioactivity.

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《Journal of Medicinal Chemistry》 |2023年第10期|6523-6541|共19页
作者
Suresh Blessy M.; Taghavi Amirhossein; Childs-Disney Jessica L.Disney Matthew D.;
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UF Scripps Biomed Res;

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正文语种英语
中图分类药学;
关键词
MOLECULAR-STRUCTURE DETERMINATION; DYNAMIC COMBINATORIAL CHEMISTRY; SEQUENCE-BASED DESIGN; HEPATITIS-C VIRUS; DRUG DISCOVERY; NONCODING RNAS; LEAD DISCOVERY; XPLOR-NIH; LIGAND INTERACTIONS; RIBOSOMAL-RNA;

Fragment-Based Approaches to Identify RNA Binders

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