Major General James G. Blunt

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]

References

^ Thomas U. Mayer; Tarun M. Kapoor; Stephen J. Haggarty; Randall W. King; Stuart L. Schreiber; Timothy J. Mitchison (1999). "Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen". Science. 286 (5441): 971–974. doi:10.1126/science.286.5441.971. PMID 10542155. S2CID 15348455.
^ Maliga Z, Kapoor TM, Mitchison TJ (September 2002). "Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5". Chem. Biol. 9 (9): 989–96. doi:10.1016/S1074-5521(02)00212-0. PMID 12323373.

[1] Thomas U. Mayer; Tarun M. Kapoor; Stephen J. Haggarty; Randall W. King; Stuart L. Schreiber; Timothy J. Mitchison (1999). "Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen". Science. 286 (5441): 971–974. doi:10.1126/science.286.5441.971. PMID 10542155. S2CID 15348455.

[2] Maliga Z, Kapoor TM, Mitchison TJ (September 2002). "Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5". Chem. Biol. 9 (9): 989–96. doi:10.1016/S1074-5521(02)00212-0. PMID 12323373.

[1]

[2]