Carbonic anhydrase inhibitor coated gold nanoparticles selectively inhibit the tumor-associated isoform IX over the cytosolic isozymes I and II.
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.
Stiti
Maamar
M
Institut des Biomolécules Max Mousseron UMR 5247 CNRS-UM1-UM2 Ecole Nationale Supérieure de Chimie de Montpellier, Montpellier Cedex, France.
Cecchi
Alessandro
A
Rami
Marouan
M
Abdaoui
Mohamed
M
Barragan-Montero
Véronique
V
Scozzafava
Andrea
A
Guari
Yannick
Y
Winum
Jean-Yves
JY
Supuran
Claudiu T
CT
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
D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D006046:Gold; D002256:Carbonic Anhydrases