Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors

• Verfasst von: Altmeyer, Markus [VerfasserIn]
• Verfasst von: Marschner, Aline [VerfasserIn]
• Verfasst von: Schiffmann, Rolf [VerfasserIn]
• Verfasst von: Klein, Christian D. [VerfasserIn]
• Titel: Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors
• Verf.angabe: Markus A. Altmeyer, Aline Marschner, Rolf Schiffmann, Christian D. Klein
• E-Jahr: 2010
• Jahr: 27 May 2010
• Umfang: 7 S.
• Fussnoten: Gesehen am 22.11.2022
• Titel Quelle: Enthalten in: Bioorganic & medicinal chemistry letters
• Ort Quelle: Amsterdam [u.a.] : Elsevier Science, 1991
• Jahr Quelle: 2010
• Band/Heft Quelle: 20(2010), 14, Seite 4038-4044
• ISSN Quelle: 1464-3405
• DOI: doi:10.1016/j.bmcl.2010.05.093
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: Benzimidazole
• Sach-SW: Hydroxyquinoline
• Sach-SW: Methionine aminopeptidase
• Sach-SW: Picolinic acid
• Sach-SW: Selectivity
• K10plus-PPN: 1823170358

Abstract

Inhibitors of methionine aminopeptidases (MetAPs) are treatment options for various pathological conditions. Several inhibitor classes have been described previously, but only few data on the subtype selectivity, which is of crucial importance for these enzymes, is available. We present a systematic study on the subtype- and species-selectivity of MetAP inhibitors that require the binding of an auxiliary metal ion. This includes, in particular, compounds based on the benzimidazole pharmacophore, but also hydroxyquinoline and picolinic acid derivatives. Our data indicates that a significant degree of selectivity can be attained with metal-dependent MetAP inhibitors.