Monastrol Explained

Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab of Tim Mitchison. Monastrol was shown to inhibit the kinesin-5 (also known as KIF11, Kinesin Eg5), a motor protein important for spindle bipolarity.^[1]

Mechanism of action

Monastrol binds to a long loop that is specific to the Eg5 (also known as KIF11 or kinesin-5) kinesin family, and allosterically inhibits ATPase activity of the kinesin ^[2]

Notes and References

1. Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen . Thomas U. Mayer . Tarun M. Kapoor . Stephen J. Haggarty . Randall W. King . Stuart L. Schreiber . Timothy J. Mitchison . Science . 1999 . 286 . 5441 . 971–974 . 10542155 . 10.1126/science.286.5441.971. 15348455 .
2. Maliga Z, Kapoor TM, Mitchison TJ . Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5 . Chem. Biol. . 9 . 9 . 989–96 . September 2002 . 12323373 . 10.1016/S1074-5521(02)00212-0 . free .