CRYSTAL STRUCTURE OF THE PRO FORM OF A MATRIX METALLOPROTEINASE AND AN ALLOSTERIC PROCESSING INHIBITOR

The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit th...

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Hauptverfasser:	TOUNGE, Brett, A, LEWANDOWSKI, Frank, A, MAGUIRE, Diane, M, WANG, Aihua, MILLIGAN, Cynthia, M, TODD, Matthew, J, DECKMAN, Ingrid, Christa, BONE, Roger, F, SCHALK-HIHI, Celine, JACKSON, Paul, F, ALEXANDER, Richard, Scott, SCANNEVIN, Robert, H, SPRINGER, Barry, SPURLINO, John, C, LEONARD, Kristi, A, RHODES, Kenneth, J, BARBAY, Joseph, Kent, KUO, Lawrence, C
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	BEER BIOCHEMISTRY CALCULATING CHEMISTRY COMPOSITIONS THEREOF COMPUTING COUNTING CULTURE MEDIA ELECTRIC DIGITAL DATA PROCESSING ENZYMOLOGY METALLURGY MICROBIOLOGY MICROORGANISMS OR ENZYMES MUTATION OR GENETIC ENGINEERING PHYSICS PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS SPIRITS VINEGAR WINE
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Beschreibung
Zusammenfassung:	The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.