title: Selective targeting of tumor and stromal cells by a nanocarrier system displaying lipidated cathepsin B inhibitor.
abstract: Cathepsin B (CtsB) is a lysosomal cysteine proteinase that is specifically translocated to the extracellular milieu during cancer progression. The development of a lipidated CtsB inhibitor incorporated into the envelope of a liposomal nanocarrier (LNC-NS-629) is described. Ex vivo and in vivo studies confirmed selective targeting and internalization of LNC-NS-629 by tumor and stromal cells, thus validating CtsB targeting as a highly promising approach to cancer diagnosis and treatment.
authors: Department of Biochemistry and Molecular and Structural Biology, Jozef Stefan Institute, 1000 Ljubljana (Slovenia); National Research Tomsk Polytechnic University, 634050 Tomsk (Russia); Jozef Stefan International Postgraduate School, 1000 Ljubljana (Slovenia).
authors: G
authors: G
authors: Mikhaylov
authors: D
authors: D
authors: Klimpel
authors: N
authors: N
authors: Schaschke
authors: U
authors: U
authors: Mikac
authors: M
authors: M
authors: Vizovisek
authors: M
authors: M
authors: Fonovic
authors: V
authors: V
authors: Turk
authors: Boris
authors: B
authors: Turk
authors: Olga
authors: O
authors: Vasiljeva
mesh_terms: D000818:Animals; D002401:Cathepsin B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002471:Cell Transformation, Neoplastic / Q000187:drug effects* / Q000473:pathology; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005260:Female; D008325:Mammary Neoplasms, Experimental / Q000175:diagnosis / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D049329:Nanostructures / Q000737:chemistry*; D014411:Neoplastic Stem Cells / Q000187:drug effects* / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D015853:Cysteine Proteinase Inhibitors; D004337:Drug Carriers; D004317:Doxorubicin; D002401:Cathepsin B
keywords: cancer; cathepsin B; drug delivery; theranostics; tumor microenvironment