Title of article
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors
Author/Authors
Anne-Claude Dublanchet، نويسنده , , Pierre Ducrot، نويسنده , , Charles Andrianjara، نويسنده , , Margaret O’Gara، نويسنده , , Renaud Morales، نويسنده , , Delphine Compère، نويسنده , , Alexis Denis، نويسنده , , Stéphane Blais، نويسنده , , Philippe Cluzeau، نويسنده , , Karine Courté، نويسنده , , Jacques Hamon، نويسنده , , François Moreau-Gaudry، نويسنده , , Marie-Laure Prunet، نويسنده , , Anita Tertre، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
3787
To page
3790
Abstract
A new class of MMP-12 inhibitors was discovered and optimized using structure-based drug design methods. Modeling studies using a known MMP-12 crystal structure identified a new interaction mode for these new MMP-12 inhibitors. Further optimization resulted in the discovery of a compound displaying nanomolar activity against MMP-12 and which was co-crystallized with MMP-12.
Keywords
Matrix metalloprotease 12 , Human metalloelastase , Non-zinc chelating inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795881
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