title: In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives.
abstract: We describe the synthesis and characterization of two acetazolamide derivatives containing either a charged fluorophore or an albumin-binding moiety, which restrict binding to carbonic anhydrase IX and XII present on tumor cells. In vivo studies showed the preferentially targeting of tumor cells by the fluorescent acetazolamide derivative and the ability of the albumin-binding acetazolamide derivative to cause tumor retardation in a SK-RC-52 xenograft model of cancer.
authors.affiliation: Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zurich, CH-8093 Zurich, Switzerland.
authors.forename: Julia K J
authors.initials: JK
authors.lastname: Ahlskog
authors.forename: Christoph E
authors.initials: CE
authors.lastname: Dumelin
authors.forename: Sabrina
authors.initials: S
authors.lastname: Trüssel
authors.forename: Jessica
authors.initials: J
authors.lastname: Mårlind
authors.forename: Dario
authors.initials: D
authors.lastname: Neri
mesh_terms: D000081:Acetamides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000951:Antigens, Neoplasm / Q000737:chemistry / Q000378:metabolism*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D000071231:Carbonic Anhydrase IX; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000737:chemistry / Q000378:metabolism*; D045744:Cell Line, Tumor; D015179:Colorectal Neoplasms / Q000188:drug therapy / Q000201:enzymology; D005456:Fluorescent Dyes / Q000737:chemistry; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D023041:Xenograft Model Antitumor Assays
chemical_list: D000081:Acetamides; D000951:Antigens, Neoplasm; D000970:Antineoplastic Agents; D002257:Carbonic Anhydrase Inhibitors; D005456:Fluorescent Dyes; C089226:CA9 protein, human; D000071231:Carbonic Anhydrase IX; D002256:Carbonic Anhydrases; C477378:carbonic anhydrase XII