Plant specialised metabolites constitute an enormous reservoir of anticancer compounds.
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Their low bioavailability in planta fails to reach the demand.
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Heterologous pathway reconstitution is a promising alternative to massively producing these compounds.
The discovery and supply of plant-derived anti-cancer compounds remain challenging given their low bioavailability and structural complexity. Reconstituting the pathways of these compounds in heterologous hosts is a promising solution; however, requires the complete elucidation of the biosynthetic genes involved and extensive metabolic engineering to optimise enzyme activity and metabolic flux. This review describes the current strategies and recent advancements in the production of these valuable therapeutic compounds, and highlights plant-derived immunomodulators as an emerging class of anti-cancer agents.