{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,8]],"date-time":"2026-05-08T11:10:11Z","timestamp":1778238611200,"version":"3.51.4"},"reference-count":330,"publisher":"MDPI AG","issue":"22","license":[{"start":{"date-parts":[[2020,11,14]],"date-time":"2020-11-14T00:00:00Z","timestamp":1605312000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100000780","name":"European Commission","doi-asserted-by":"publisher","award":["764837"],"award-info":[{"award-number":["764837"]}],"id":[{"id":"10.13039\/501100000780","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001871","name":"Funda\u00e7\u00e3o para a Ci\u00eancia e a Tecnologia","doi-asserted-by":"publisher","award":["MedChemTrain PhD programme"],"award-info":[{"award-number":["MedChemTrain PhD programme"]}],"id":[{"id":"10.13039\/501100001871","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Photodynamic therapy (PDT) is a promising cancer treatment which involves a photosensitizer (PS), light at a specific wavelength for PS activation and oxygen, which combine to elicit cell death. While the illumination required to activate a PS imparts a certain amount of selectivity to PDT treatments, poor tumor accumulation and cell internalization are still inherent properties of most intravenously administered PSs. As a result, common consequences of PDT include skin photosensitivity. To overcome the mentioned issues, PSs may be tailored to specifically target overexpressed biomarkers of tumors. This active targeting can be achieved by direct conjugation of the PS to a ligand with enhanced affinity for a target overexpressed on cancer cells and\/or other cells of the tumor microenvironment. Alternatively, PSs may be incorporated into ligand-targeted nanocarriers, which may also encompass multi-functionalities, including diagnosis and therapy. In this review, we highlight the major advances in active targeting of PSs, either by means of ligand-derived bioconjugates or by exploiting ligand-targeting nanocarriers.<\/jats:p>","DOI":"10.3390\/molecules25225317","type":"journal-article","created":{"date-parts":[[2020,11,16]],"date-time":"2020-11-16T22:48:47Z","timestamp":1605566927000},"page":"5317","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":81,"title":["Ligand-Targeted Delivery of Photosensitizers for Cancer Treatment"],"prefix":"10.3390","volume":"25","author":[{"given":"Piotr","family":"Gierlich","sequence":"first","affiliation":[{"name":"CQC, Coimbra Chemistry Center, Department of Chemistry, University of Coimbra, 3000-435 Coimbra, Portugal"},{"name":"Medicinal Chemistry, Trinity Translational Medicine Institute, Trinity Centre for Health Sciences, Trinity College Dublin, The University of Dublin, St. James\u2019s Hospital, D08W9RT Dublin, Ireland"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9508-7035","authenticated-orcid":false,"given":"Ana I.","family":"Mata","sequence":"additional","affiliation":[{"name":"CQC, Coimbra Chemistry Center, Department of Chemistry, University of Coimbra, 3000-435 Coimbra, Portugal"}]},{"given":"Claire","family":"Donohoe","sequence":"additional","affiliation":[{"name":"CQC, Coimbra Chemistry Center, Department of Chemistry, University of Coimbra, 3000-435 Coimbra, Portugal"},{"name":"Medicinal Chemistry, Trinity Translational Medicine Institute, Trinity Centre for Health Sciences, Trinity College Dublin, The University of Dublin, St. James\u2019s Hospital, D08W9RT Dublin, Ireland"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9128-2557","authenticated-orcid":false,"given":"Rui M. M.","family":"Brito","sequence":"additional","affiliation":[{"name":"CQC, Coimbra Chemistry Center, Department of Chemistry, University of Coimbra, 3000-435 Coimbra, Portugal"},{"name":"BSIM Therapeutics, Instituto Pedro Nunes, 3030-199 Coimbra, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7467-1654","authenticated-orcid":false,"given":"Mathias O.","family":"Senge","sequence":"additional","affiliation":[{"name":"Medicinal Chemistry, Trinity Translational Medicine Institute, Trinity Centre for Health Sciences, Trinity College Dublin, The University of Dublin, St. James\u2019s Hospital, D08W9RT Dublin, Ireland"}]},{"given":"L\u00edgia C.","family":"Gomes-da-Silva","sequence":"additional","affiliation":[{"name":"CQC, Coimbra Chemistry Center, Department of Chemistry, University of Coimbra, 3000-435 Coimbra, Portugal"}]}],"member":"1968","published-online":{"date-parts":[[2020,11,14]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"451","DOI":"10.1016\/j.jconrel.2014.03.057","article-title":"EPR: Evidence and fallacy","volume":"190","author":"Nichols","year":"2014","journal-title":"J. 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