ReviewRSC advances2026
Therapeutic horizons in the development of PROTAC-based EZH2 inhibitors: recent achievements, comparative analysis, and future perspectives.
Review in RSC advances, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Abstract
EZH2, a histone methyltransferase and the catalytic subunit of the polycomb repressive complex 2 (PRC2), plays a pivotal role in tumor epigenetics through transcriptional repression of tumor suppressor genes. Despite the clinical success of tazemetostat, classical small-molecule inhibitors face limitations related to incomplete target occupancy, adaptive resistance, and non-catalytic EZH2 functions. These challenges have driven a paradigm shift toward proteolysis-targeting chimeras (PROTACs)-bifunctional molecules that inhibit EZH2 through E3 ligase-mediated ubiquitination and proteasomal degradation. This review discusses the design principles, synthetic approaches, structural diversity, and pharmacological profiles of recently developed VHL-, CRBN-, and cIAP-recruiting EZH2 inhibitors reported in the last five years. Comparative analysis of enzymatic inhibition, cellular cytotoxicity, and degradation kinetics highlights MS8847 (84) as a verified degrader (DC
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