Abstract:
:Matrix metalloproteinases (MMPs) are a family of zinc endopeptidases that have been implicated in various disease processes. Different classes of MMP inhibitors, including hydroxamic acids, phosphinic acids and thiols, have been previously described. Most of these mimic peptides and most likely bind in a similar way to the corresponding peptide substrates. Here we describe pyrimidine-triones as a completely new class of metalloprotease inhibitors. While the pyrimidine-trione template is used as the zinc-chelating moiety, the substituents have been optimized to yield inhibitors comparable in their inhibition efficiency of matrix metalloproteinases to hydroxamic acid derivatives such as batimastat. However, they are much more specific for a small subgroup of MMPs, namely the gelatinases (MMP-2 and MMP-9).
journal_name
Biol Chemjournal_title
Biological chemistryauthors
Grams F,Brandstetter H,D'Alò S,Geppert D,Krell HW,Leinert H,Livi V,Menta E,Oliva A,Zimmermann G,Gram F,Brandstetter H,D'Alò S,Geppert D,Krell HW,Leinert H,Livi VMenta E,Oliva A,Zimmermann Gdoi
10.1515/BC.2001.159keywords:
subject
Has Abstractpub_date
2001-08-01 00:00:00pages
1277-85issue
8eissn
1431-6730issn
1437-4315journal_volume
382pub_type
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