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In recent years, research on the therapeutic potential of mushroom species has notably expanded, and the effects of these organisms on cancer treatment have come to the forefront. The present review examines the anticancer and antitumor effects of various edible and medicinal mushroom species on different human cancer cell lines and summarizes the biological mechanisms underlying these effects. The reviewed studies show that polysaccharides (particularly β-glucans), triterpenoids, phenolic compounds, protein-polysaccharide complexes and other bioactive components contained in mushrooms are effective on apoptosis induction, cell cycle arrest, activation of the immune system, reduction of oxidative stress, inhibition of metastasis and angiogenesis. In vitro and in vivo studies, especially on species such as Ganoderma lucidum, Cordyceps militaris, Lentinula edodes, Hericium erinaceus, and Grifola frondosa, have shown that these mushrooms exhibit significant cytotoxic, antiproliferative, and immunomodulatory effects against various types of cancer (including breast, colon, lung, liver, prostate, cervical, etc.). These findings indicate that mushroom-derived natural products should be evaluated not only as adjunctive therapies, but also as potential pharmaceutical agents. However, most of the available data are at the preclinical level, and more comprehensive toxicological and pharmacokinetic studies are needed to ensure clinical applicability.