Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors
摘要:
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. (C) 2010 Elsevier Ltd. All rights reserved.
Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors
作者:Markus A. Altmeyer、Aline Marschner、Rolf Schiffmann、Christian D. Klein
DOI:10.1016/j.bmcl.2010.05.093
日期:2010.7
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. (C) 2010 Elsevier Ltd. All rights reserved.