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Its diverse molecular composition, including neurotoxins, antimicrobial peptides, and enzymes, provides a vast library for therapeutic innovation. Proteomic analyses have characterized venom composition in several species, while further functional assays have clarified their anticancer mechanisms. This review synthesizes current knowledge on scorpion venom-derived peptides with demonstrated anticancer activity, which selectively target ion channels, induce apoptosis, or disrupt tumor microenvironments. Where available, we highlight proteomic studies that have identified these components and discuss their structural features relevant to drug design. We also examine clinical applications and the challenges in translating venom peptides into therapies. The crucial and growing role of proteomics in this field, particularly for venom fractionation, component identification, and structural characterization, is critically evaluated.<\/jats:p>","DOI":"10.3390\/ijms26209907","type":"journal-article","created":{"date-parts":[[2025,10,17]],"date-time":"2025-10-17T16:13:03Z","timestamp":1760717583000},"page":"9907","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Scorpion Venom as a Source of Cancer Drugs: A Comprehensive Proteomic Analysis and Therapeutic Potential"],"prefix":"10.3390","volume":"26","author":[{"given":"Stephanie Santos Suehiro","family":"Arcos","sequence":"first","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mariana Ramos da Cunha","family":"Aguiar","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"J\u00falia de","family":"Oliveira","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Matheus Ramos da","family":"Silva","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Isabela de Oliveira Cavalcante","family":"Pimentel","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nicolas Gamboa","family":"dos Anjos","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gustavo Henrique Rohr Souza","family":"Machado","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kimberly Borges","family":"Evangelista","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9582-4699","authenticated-orcid":false,"given":"Fernanda Calheta Vieira","family":"Portaro","sequence":"additional","affiliation":[{"name":"Laboratory of Structure and Functions of Biomolecules, Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1571-7763","authenticated-orcid":false,"given":"Leo Kei","family":"Iwai","sequence":"additional","affiliation":[{"name":"Laboratory of Applied Toxinology (LETA) and Center of Toxins, Immune-Response and Cell Signaling (CeTICS), Butantan Institute, S\u00e3o Paulo 05503-900, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2025,10,11]]},"reference":[{"key":"ref_1","first-page":"229","article-title":"Global Cancer Statistics 2022: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries","volume":"74","author":"Bray","year":"2024","journal-title":"CA Cancer J. 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