[HTML][HTML] Development of selective inhibitors and substrate of matrix metalloproteinase-12
L Devel, V Rogakos, A David, A Makaritis… - Journal of Biological …, 2006 - ASBMB
Four phosphinic peptide libraries with compounds having the general formula p-Br-Ph-(PO 2-
CH 2)-Xaa′-Yaa′-Zaa′-NH 2 have been prepared and screened against 10 matrix
metalloproteinases (MMPs). We identified two phosphinic peptides with K i values of 0.19
and 4.4 nm toward MMP-12 (macrophage elastase) that are more than 2-3 orders of
magnitude less potent toward the other MMPs tested. These highly selective MMP-12
inhibitors contain a Glu-Glu motif in their Yaa′-Zaa′ positions. Incorporation of this Glu …
CH 2)-Xaa′-Yaa′-Zaa′-NH 2 have been prepared and screened against 10 matrix
metalloproteinases (MMPs). We identified two phosphinic peptides with K i values of 0.19
and 4.4 nm toward MMP-12 (macrophage elastase) that are more than 2-3 orders of
magnitude less potent toward the other MMPs tested. These highly selective MMP-12
inhibitors contain a Glu-Glu motif in their Yaa′-Zaa′ positions. Incorporation of this Glu …