title: A marine natural product inhibitor of kinesin motors.
abstract: Members of the kinesin superfamily of motor proteins are essential for mitotic and meiotic spindle organization, chromosome segregation, organelle and vesicle transport, and many other processes that require microtubule-based transport. A compound, adociasulfate-2, was isolated from a marine sponge, Haliclona (also known as Adocia) species, that inhibited kinesin activity by targeting its motor domain and mimicking the activity of the microtubule. Thus, the kinesin-microtubule interaction site could be a useful target for small molecule modulators, and adociasulfate-2 should serve as an archetype for specific inhibitors of kinesin functions.
authors.affiliation: Department of Pharmacology, Division of Cellular and Molecular Medicine, Howard Hughes Medical Institute, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0683, USA.
authors.forename: R
authors.initials: R
authors.lastname: Sakowicz
authors.forename: M S
authors.initials: MS
authors.lastname: Berdelis
authors.forename: K
authors.initials: K
authors.lastname: Ray
authors.forename: C L
authors.initials: CL
authors.lastname: Blackburn
authors.forename: C
authors.initials: C
authors.lastname: Hopmann
authors.forename: D J
authors.initials: DJ
authors.lastname: Faulkner
authors.forename: L S
authors.initials: LS
authors.lastname: Goldstein
mesh_terms: D000244:Adenosine Diphosphate / Q000378:metabolism; D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors; D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D001665:Binding Sites; D002455:Cell Division / Q000187:drug effects; D004330:Drosophila / Q000196:embryology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D016547:Kinesins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007700:Kinetics; D008870:Microtubules / Q000378:metabolism*; D008938:Mitosis / Q000187:drug effects; D011161:Porifera / Q000737:chemistry*; D013463:Sulfuric Acid Esters / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D013463:Sulfuric Acid Esters; C111568:adociasulfate-2; D000244:Adenosine Diphosphate; D000255:Adenosine Triphosphate; D000251:Adenosine Triphosphatases; D016547:Kinesins