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Its overexpression is frequently observed in aggressive cancers such as breast cancer, melanoma, and glioma, where it drives tumor growth, metastasis, and resistance to oxidative stress. Targeting PHGDH with small\u2010molecule inhibitors has emerged as a promising therapeutic strategy. Notable inhibitors like NCT\u2010503, CBR\u20105884, Azacoccone E, and Ixocarpalactone A, along with covalent inhibitors such as Withangulatin A, exhibit potent anticancer activity by limiting serine availability and inducing apoptosis. Gene\u2010silencing techniques, including RNA interference (RNAi) and CRISPR\/Cas9, further validate PHGDH as a therapeutic target. Advances in computational methods and structure\u2013activity relationship (SAR) analysis have accelerated the discovery of selective PHGDH inhibitors, offering insights into binding mechanisms and facilitating rational drug design. 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