You are here
The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells.
| Title: | The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells. |
 99 views 40 downloads |
|---|---|---|
| Name(s): |
Kowalski, R. J. Giannakakou, P. Gunasekera, Sarath P. Longley, Ross E. Day, B. W. Hamel, E. Harbor Branch Oceanographic Institute |
|
| Type of Resource: | text | |
| Genre: | Article | |
| Date Issued: | 1997 | |
| Publisher: | American Society for Pharmacology and Experimental Therapeutics | |
| Place of Publication: | Baltimore, MD | |
| Physical Form: | ||
| Extent: | 11 p. | |
| Language(s): | English | |
| Identifier: | FA00007052 (IID), 10.1124/mol.52.4.613 (doi) | |
| Note(s): |
The lactone-bearing polyhydroxylated alkatetraene (+)-discodermolide, which was isolated from the sponge Discodermia dissoluta, induces the polymerization of purified tubulin with and without microtubule-associated proteins or GTP, and the polymers formed are stable to cold and calcium. These effects are similar to those of paclitaxel (Taxol), but discodermolide is more potent. We confirmed that these properties represent hypernucleation phenomena; we obtained lower tubulin critical concentrations and shorter polymers with discodermolide than paclitaxel under a variety of reaction conditions. Florida Atlantic University. Harbor Branch Oceanographic Institute contribution 1202 This manuscript is an author version with the final publication available and may be cited as: Kowalski, R. J., Giannakakou, P., Gunasekera, S. P., Longley, R. E., Day, B. W., & Hamel, E. (1997). The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells. Molecular Pharmacology, 52(4), 613-622. |
|
| Subject(s): |
Marine natural products Cytotoxins Tubulin Modulators Paclitaxel Lactones Sponges |
|
| Links: | http://dx.doi.org/10.1124/mol.52.4.613 | |
| Persistent Link to This Record: | http://purl.flvc.org/fau/fd/FA00007052 | |
| Host Institution: | FAU |
