October 10, 2007Chemical Biology & Drug Design

Metabolism of a Highly Selective Gelatinase Inhibitor Generates Active Metabolite

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Population

In vitro systems (matrix metalloproteinases 2, 9, and 14)

Design

Preclinical

Authors

MLMijoon LeeUniversity of Notre Dame AVAdriel Villegas‐EstradaCornell University GCGiuseppe CelenzaUniversity of L'Aquila

Discussion

Member takes

Implication

Animal metabolite data should not inform clinical gelatinase inhibitor use; leaves open metabolite contributions to MMP-2/9/14 inhibition in preclinical models.

Structured PICO

Population

In vitro systems (matrix metalloproteinases 2, 9, and 14)

Intervention

(4-Phenoxyphenylsulfonyl)methylthiirane (inhibitor 1) and its metabolite 4-(4-thiiranylmethanesulfonylphenoxy)phenol (compound 21)

Outcome

Identification of metabolites and kinetics of inhibition of matrix metalloproteinasessurrogate

The in vivo activity of the selective gelatinase inhibitor 1 is likely driven by its active metabolite, compound 21, which is a more potent inhibitor of MMP-2, MMP-9, and MMP-14.

Cite This Study

Lee et al. (2007) studied this question.

synapsesocial.com/papers/6a8ce623748301e7973019f3 https://doi.org/10.1111/j.1747-0285.2007.00577.x

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Implication

Animal metabolite data should not inform clinical gelatinase inhibitor use; leaves open metabolite contributions to MMP-2/9/14 inhibition in preclinical models.