JNJ0966 is a potent and highly selective inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation. It appears that JNJ0966 binds to a structural pocket in proximity to the MMP-9 zymogen cleavage site near Arg-106. JNJ0966 reduces disease severity in in a mouse experimental autoimmune encephalomyelitis (EAE) model. JNJ0966 does not inhibit activation of MMP-2 zymogen, and has no effect on MMP-1, MMP-2, MMP-3, MMP-9 or MMP-14 catalytic activity.
potent and highly selective inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation
The Journal of biological chemistry, 292(43), 17963-17974 (2017-09-02)
Aberrant activation of matrix metalloproteinases (MMPs) is a common feature of pathological cascades observed in diverse disorders, such as cancer, fibrosis, immune dysregulation, and neurodegenerative diseases. MMP-9, in particular, is highly dynamically regulated in several pathological processes. Development of MMP
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