Kinesin motor modulators derived from the marine sponge Adocia
AssigneeThe Regents of the University of California
InventorsLawrence S.B. Goldstein, David John Faulkner, Roman Sakowicz, Michael S. Berdelis, Christine L. Blackburn, Cordula Hopmann
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Abstract
This invention provides novel compounds derived from a marine sponge, Adocia sp., that specifically modulat kinesin activity by targeting the kinesin motor domain and mimicking the activity a microtubule. The compounds act as potent anti-mitogens are useful in a wide variety of in vitro and in vivo applications.
Claims17
A method of modulating kinesin motor activity, said method comprising contacting said kinesin motor with a molecule that competitively inhibits said kinesin motor at a microtubule binding site, wherein said molecule is identified according to the following steps:
- (i) assaying for competitive inhibition of said kinesin motor activity by said molecule at a kinesin ATPase site;
- (ii) assaying for competitive inhibition of said kinesin motor activity by said molecule at a microtubule binding site;
- and
- (iii) identifying said molecule as a kinesin modulator specific to a microtubule binding site when said molecule is a competitive modulator at said microtubule binding site, but not at said ATPase site.
Dependencies are inferred from the claim text.