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Notably, RNA can form intricate three\u2010dimensional structures, and their biological functions are dependent on these structures. Targeting the structured regions of RNA with small molecules has gained increasing attention over the past decade, because it provides both chemical probes to study fundamental biology processes and lead medicines for diseases with unmet medical needs. Recent advances in RNA structure prediction and determination and RNA biology have accelerated the rational design and development of RNA\u2010targeted small molecules to modulate disease pathology. However, challenges remain in advancing RNA\u2010targeted small molecules towards clinical applications. This review summarizes strategies to study RNA structures, to identify small molecules recognizing these structures, and to augment the functionality of RNA\u2010binding small molecules. We focus on recent advances in developing RNA\u2010targeted small molecules as potential therapeutics in a variety of diseases, encompassing different modes of actions and targeting strategies. 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