The development and application of small molecule modulators of SF3b as therapeutic agents for cancer

► Details the potential of developing the spliceosome as an anticancer target. ► Reviews currently available natural product and synthetic spliceosome modulators. ► Discusses the role of alternative splicing in cancer therapy. ► Reviews the selective antitumor activity of spliceosomal targeting agents. ► Elucidates potential mechanisms of cytotoxicity induced by spliceosome modulators.