Title of article :
Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8 Original Research Article
Author/Authors :
Gianluca Bianchini، نويسنده , , Massimiliano Aschi، نويسنده , , Giancarlo Cavicchio، نويسنده , , Marcello Crucianelli، نويسنده , , Serena Preziuso، نويسنده , , Carlo Gallina، نويسنده , , Adele Nastari، نويسنده , , Enrico Gavuzzo، نويسنده , , Fernando Mazza، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
Abstract :
Three novel peptidomimetic phosphinate inhibitors have been synthesized and evaluated as inhibitors of matrix metalloproteinases MMP-2 and MMP-8. Their IC50 values are in the micromolar range, and one of them showed to be the most effective inhibitor of MMP-2. The differences in binding affinities for MMP-2 and MMP-8 of the three phosphinates have been rationalized by means of modelling studies and molecular dynamics simulations.
Keywords :
Matrix metalloproteinases inhibitors , Phosphinic acids , peptidomimetics , Molecular dynamics and modelling
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry
