Photodynamic　therapy　(PDT)　has　attracted　much　interest　for　the　treatment　of　cancer　due　to　the　increased　incidence　of　multidrug　resistance　and　systemic　toxicity　in　conventional　chemotherapy.　Phthalocyanine　(Pc)　is　one　of　main　classes　of　photosensitizers　for　PDT　and　possesses　optimal　photophysical　and　photochemical　properties.　A　higher　specificity　can　ideally　be　achieved　when　Pcs　are　targeted　towards　tumor-specific　receptors,　which　may　also　facilitate　specific　drug　delivery.　Herein,　we　develop　a　simple　and　unique　strategy　to　prepare　a　hydrophilic　tumor-targeting　photosensitizer　ATF-ZnPc　by　covalently　coupling　zinc　phthalocyanine　(ZnPc)　to　the　amino-terminal　fragment　(ATF)　of　urokinase-type　plasminogen　activator　(uPA),　a　fragment　responsible　for　uPA　receptor　(uPAR,　a　biomarker　overexpressed　in　cancer　cells),　through　the　carboxyl　groups　of　ATF.　We　demonstrate　the　high　efficacy　of　this　tumor-targeting　PDT　agent　for　the　inhibition　of　tumor　growth　both　in　vitro　and　in　vivo.　Our　in　vivo　optical　imaging　results　using　H22　tumor-bearing　mice　show　clearly　the　selective　accumulation　of　ATF-ZnPc　in　tumor　region,　thereby　revealing　the　great　potential　of　ATF-ZnPc　for　clinical　applications　such　as　cancer　detection　and　guidance　of　tumor　resection　in　addition　to　photodynamic　treatment.　©　2014　Acta　Materialia　Inc.