title: Carbonic anhydrase inhibitor coated gold nanoparticles selectively inhibit the tumor-associated isoform IX over the cytosolic isozymes I and II.
abstract: An approach for the synthesis of carbonic anhydrase (CA, EC 4.2.1.1) inhibitor coated gold nanoparticles is reported. This nanomaterial selectively inhibited the tumor-associated isoform CA IX overexpressed in hypoxic cancers over the ubiquitous, cytosolic housekeeping isozymes CA I and II and was membrane impermeant. As CA IX has an extracellular active site, the new nanomaterial which is confined to the extracellular space may be useful for imaging and treatment of hypoxic tumors.
authors.affiliation: Institut des Biomolécules Max Mousseron UMR 5247 CNRS-UM1-UM2 Ecole Nationale Supérieure de Chimie de Montpellier, Montpellier Cedex, France.
authors.forename: Maamar
authors.initials: M
authors.lastname: Stiti
authors.forename: Alessandro
authors.initials: A
authors.lastname: Cecchi
authors.forename: Marouan
authors.initials: M
authors.lastname: Rami
authors.forename: Mohamed
authors.initials: M
authors.lastname: Abdaoui
authors.forename: Véronique
authors.initials: V
authors.lastname: Barragan-Montero
authors.forename: Andrea
authors.initials: A
authors.lastname: Scozzafava
authors.forename: Yannick
authors.initials: Y
authors.lastname: Guari
authors.forename: Jean-Yves
authors.initials: JY
authors.lastname: Winum
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000378:metabolism*; D003600:Cytosol / Q000187:drug effects / Q000201:enzymology*; D006046:Gold / Q000737:chemistry*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D053768:Metal Nanoparticles / Q000737:chemistry*; D015394:Molecular Structure; D009369:Neoplasms / Q000201:enzymology*; D013379:Substrate Specificity
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D006046:Gold; D002256:Carbonic Anhydrases