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The development of cancer-specific diagnostic agents and anticancer toxins would improve patient survival. The current and standard types of medical care for cancer patients, including surgery, radiotherapy, and chemotherapy, are not able to treat all cancers. A new treatment strategy utilizing tumor targeting peptides to selectively deliver drugs or applicable active agents to solid tumors is becoming a promising approach. In this review, we discuss the different tumor-homing peptides discovered through combinatorial library screening, as well as native active peptides. The different structure\u2013function relationship data that have been used to improve the peptide\u2019s activity and conjugation strategies are highlighted.<\/jats:p>","DOI":"10.3390\/pharmaceutics13040481","type":"journal-article","created":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T23:05:11Z","timestamp":1617318311000},"page":"481","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":64,"title":["Peptide-Based Strategies for Targeted Tumor Treatment and Imaging"],"prefix":"10.3390","volume":"13","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-4173-162X","authenticated-orcid":false,"given":"Abiodun","family":"Ayo","sequence":"first","affiliation":[{"name":"Translational Cancer Medicine Research Program, Faculty of Medicine, University of Helsinki, 00014 Helsinki, Finland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9620-095X","authenticated-orcid":false,"given":"Pirjo","family":"Laakkonen","sequence":"additional","affiliation":[{"name":"Translational Cancer Medicine Research Program, Faculty of Medicine, University of Helsinki, 00014 Helsinki, Finland"},{"name":"Laboratory Animal Center, HiLIFE\u2014Helsinki Institute of Life Science, University of Helsinki, 00014 Helsinki, Finland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2021,4,2]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"223","DOI":"10.1146\/annurev-anchem-091719-024553","article-title":"Mass Spectrometry of Human Transporters","volume":"13","author":"Achour","year":"2020","journal-title":"Annual Rev. 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