发明名称 |
Crystal Structure of the Pro Form of a Matrix Metalloproteinase and an Allosteric Processing Inhibitor |
摘要 |
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.
|
申请公布号 |
US2013166268(A1) |
申请公布日期 |
2013.06.27 |
申请号 |
US201213533201 |
申请日期 |
2012.06.26 |
申请人 |
LEONARD KRISTI A.;ALEXANDER RICHARD SCOTT;BARBAY JOSEPH KENT;BONE ROGER F.;DECKMAN INGRID CHRISTA;JACKSON PAUL F.;KUO LAWRENCE C.;LEWANDOWSKI FRANK A.;MAGUIRE DIANE M.;MILLIGAN CYNTHIA M.;RHODES KENNETH J.;SCANNEVIN ROBERT H.;SCHALK-HIHI CELINE;SPRINGER BARRY;SPURLINO JOHN C.;TODD MATTHEW J.;TONGUE BRETT ANDREW;WANG AIHUA |
发明人 |
LEONARD KRISTI A.;ALEXANDER RICHARD SCOTT;BARBAY JOSEPH KENT;BONE ROGER F.;DECKMAN INGRID CHRISTA;JACKSON PAUL F.;KUO LAWRENCE C.;LEWANDOWSKI FRANK A.;MAGUIRE DIANE M.;MILLIGAN CYNTHIA M.;RHODES KENNETH J.;SCANNEVIN ROBERT H.;SCHALK-HIHI CELINE;SPRINGER BARRY;SPURLINO JOHN C.;TODD MATTHEW J.;TONGUE BRETT ANDREW;WANG AIHUA |
分类号 |
G06F19/12 |
主分类号 |
G06F19/12 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|