Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8

Authors :: Bianchini G.
Aschi M.
Cavicchio G.
Crucianelli M.
Preziuso S.
Gallina C.
Nastari A.
Gavuzzo E.
Mazza F.
Source :: Bioorganic & medicinal chemistry, 13 (2005): 4740–4749., info:cnr-pdr/source/autori:Bianchini G., Aschi M., Cavicchio G., Crucianelli M., Preziuso S., Gallina C., Nastari A., Gavuzzo E., Mazza F./titolo:Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8./doi:/rivista:Bioorganic & medicinal chemistry (Print)/anno:2005/pagina_da:4740/pagina_a:4749/intervallo_pagine:4740–4749/volume:13
Publication Year :: 2005
Publisher :: Pergamon, Oxford , Regno Unito, 2005.
Abstract: Three novel peptidomimetic phosphinate inhibitors have been synthesized and evaluated as inhibitors of matrix metalloprotemases 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

Database :: OpenAIRE
Journal :: Bioorganic & medicinal chemistry, 13 (2005): 4740–4749., info:cnr-pdr/source/autori:Bianchini G., Aschi M., Cavicchio G., Crucianelli M., Preziuso S., Gallina C., Nastari A., Gavuzzo E., Mazza F./titolo:Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8./doi:/rivista:Bioorganic & medicinal chemistry (Print)/anno:2005/pagina_da:4740/pagina_a:4749/intervallo_pagine:4740–4749/volume:13
Accession number :: edsair.cnr...........7fc67824101256ed5ebaf965219e7583

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