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Journal:JBIC:15
From Proteopedia
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<b>Molecular Tour</b><br> | <b>Molecular Tour</b><br> | ||
| - | The selective inhibition of an <scene name='Journal:JBIC:15/Cv/2'>aminopeptidase from Aeromonas proteolytica (AAP)</scene>, a <scene name='Journal:JBIC:15/Cv/3'>dinuclear Zn2+</scene> hydrolase, by <scene name='Journal:JBIC:15/Cv/5'>8-quinolinol (8-hydroxyquinoline, 8-HQ)</scene> derivatives is reported. Based on our findings about 8-HQ-based Zn<sup>2+</sup> fluorophores, it was hypothesized that 8-HQ derivatives have the potential to function as specific inhibitors of Zn<sup>2+</sup> enzymes, especially dinuclear Zn<sup>2+</sup> hydrolases. Inhibitory assays of 8-HQ derivatives against AAP disclosed that the 8-HQ and 5-substituted 8-HQ′s are competitive inhibitors for AAP with inhibition constants (''K''i) of 0.16—29 μM at pH 8.0. | + | The selective inhibition of an <scene name='Journal:JBIC:15/Cv/2'>aminopeptidase from Aeromonas proteolytica (AAP)</scene>, a <scene name='Journal:JBIC:15/Cv/3'>dinuclear Zn2+</scene> hydrolase, by <scene name='Journal:JBIC:15/Cv/5'>8-quinolinol (8-hydroxyquinoline, 8-HQ)</scene> derivatives is reported. Based on our findings about 8-HQ-based Zn<sup>2+</sup> fluorophores, it was hypothesized that 8-HQ derivatives have the potential to function as specific inhibitors of Zn<sup>2+</sup> enzymes, especially dinuclear Zn<sup>2+</sup> hydrolases. Inhibitory assays of 8-HQ derivatives against AAP disclosed that the 8-HQ and 5-substituted 8-HQ′s are competitive inhibitors for AAP with inhibition constants (''K''i) of 0.16—29 μM at pH 8.0. X-ray crystal structure analysis of an AAP–8-HQ complex (1.3 Å resolution) as well as fluorescence titrations of these drugs with AAP confirmed that 8-HQ binds to AAP in the “Pyr-out” mode, in which the hydroxide anion of 8-HQ bridges two Zn<sup>2+</sup> (Zn1 and Zn2) in the active site of AAP and the nitrogen atom of 8-HQ coordinates to Zn1 (PDB code: [[3vh9]]). |
</StructureSection> | </StructureSection> | ||
Revision as of 12:08, 5 January 2012
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