A novel strategy for designing specific gelatinase A inhibitors: potential use to control tumor progression.
Matrix metalloproteases (MMPs) are zinc endopeptidases deeply implicated in tumor progression. MMP inhibitors are attractive potential anti-cancer agent. Unfortunately, until now, clinical trials remain disappointing, that could be the result of a lack of selectivity. We propose second generation selective MMPs, directed toward gelatinase A (MMP-2), based on a non-hydroxamate Zn-ligand grafted on the galardin (ilomastat) skeleton.
Augé
Franck
F
UMR CNRS 6013 "Isolement, Structures, Transformation et Synthèse de Produits Naturels", Reims Cedex, France.
Hornebeck
William
W
Laronze
Jean-Yves
JY
D000818:Animals; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020778:Matrix Metalloproteinase 2 / Q000187:drug effects / Q000378:metabolism*; D020782:Matrix Metalloproteinases / Q000502:physiology; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D020782:Matrix Metalloproteinases; D020778:Matrix Metalloproteinase 2