Exploring the Chemical and Therapeutic Potential of Fungal Secondary Metabolites for Targeted Cancer Therapy

Fungi constitute one of the most chemically rich and biologically versatile kingdoms producing an extraordinary repertoire of secondary metabolites shaped by intense ecological pressures, microbial interactions, and evolutionary innovations. These metabolites ranging from polyketides, non-ribosomal peptides, terpenoids, and alkaloids exhibit remarkable structural diversity and potent bioactivities, including cytotoxic, anti-invasive, antiangiogenic, immunomodulatory, and epigenetic effects. This book chapter explores the chemical and therapeutic potential of fungal secondary metabolites in targeted cancer therapy, emphasizing their biosynthetic origin, ecological triggers, and translational relevance. Key focus area includes the role of microbial interactions and environmental stresses in activating silent biosynthetic gene clusters; the contribution of terrestrial, endophytic, and marine fungi in producing novel anticancer scaffolds; and the immunotherapeutic potential of mushroom-derived polysaccharides. This chapter further integrates advances in genomics, metabolomics, and synthetic biology, demonstrating how metagenome mining, CRISPR-based pathway editing, and heterologous expression platforms accelerate discovery and enable rational pairing of fungal metabolites with tumor molecular subtypes. Overall, this underscores the transformative potential of fungal chemistry in developing next-generation anticancer therapeutics and drug discovery, optimization, and translational development.