Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab of

Tim Mitchison Timothy John Mitchison is a cell biologist and systems biologist and Hasib Sabbagh Professor of Systems Biology at Harvard Medical School in the United States. He is known for his discovery, with Marc Kirschner, of dynamic instability in microt ...

. Monastrol was shown to inhibit the

kinesin A kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule (MT) filaments and are powered by the hydrolysis of adenosine triphosphate (ATP) (thus kinesins are ATPases, a type of enzy ...

-5 (also known as KIF11, Kinesin Eg5), a motor protein important for spindle bipolarity.

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

References

GABAA receptor positive allosteric modulators GHB receptor agonists Thioureas Pyrimidines {{pharma-stub