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[Cancer Research 55, 2325-2333, June 1, 1995]
© 1995 American Association for Cancer Research

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Epothilones, a New Class of Microtubule-stabilizing Agents with a Taxol-like Mechanism of Action

Daniel M. Bollag, Patricia A. McQueney, Jian Zhu, Otto Hensens, Lawrence Koupal, Jerrold Liesch, Michael Goetz, Elias Lazarides1 and Catherine M. Woods2

Department of Pharmacology, Merck Research Laboratories, West Point, Pennsylvania 19486 [D. M. B., P. A. M., J. Z., E. L., C. W.] and Department of Natural Products Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065 [O. H., L. K., J. L., M. G.]

Tubulin polymerization into microtubules is a dynamic process, with the equilibrium between growth and shrinkage being essential for many cellular processes. The antineoplastic agent taxol hyperstabilizes polymerized microtubules, leading to mitotic arrest and cytotoxicity in proliferating cells. Using a sensitive filtration-calorimetric assay to detect microtubule nucleating activity, we have identified epotheliones A and B as compounds that possess all the biological effects of taxol both in vitro and in cultured cells. The epothilones are equipotent and exhibit kinetics similar to taxol in inducing tubulin polymerization into microtubules in vitro (filtration, light scattering, sedimentation, and electron microscopy) and in producing enhanced microtubule stability and bundling in cultured cells. Furthermore, these 16-membered macrolides are competitive inhibitors of [3H]taxol binding, exhibiting a 50% inhibitory concentration almost identical to that of taxol in displacement competition assays. Epothilones also cause cell cycle arrest at the G2-M transition leading to cytotoxicity, similar to taxol. In contrast to taxol, epothilones retain a much greater toxicity against P-glycoprotein-expressing multiple drug resistant cells. Epothilones, therefore, represent a novel structural class of compounds, the first to be described since the original discovery of taxol, which not only mimic the biological effects of taxol but also appear to bind to the same microtubule-binding site as taxol.

1 Present address: Astral, Inc., San Diego, CA 92121.

2 Present address: Alliance Pharmaceutical Corp., San Diego, CA 92121.

Received 1/11/95. Accepted 4/ 5/95.




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S. Goodin, M. P. Kane, and E. H. Rubin
Epothilones: Mechanism of Action and Biologic Activity
J. Clin. Oncol., May 15, 2004; 22(10): 2015 - 2025.
[Abstract] [Full Text] [PDF]


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Clin. Cancer Res.Home page
S. Mani, H. McDaid, A. Hamilton, H. Hochster, M. B. Cohen, D. Khabelle, T. Griffin, D. E. Lebwohl, L. Liebes, F. Muggia, et al.
Phase I Clinical and Pharmacokinetic Study of BMS-247550, a Novel Derivative of Epothilone B, in Solid Tumors
Clin. Cancer Res., February 15, 2004; 10(4): 1289 - 1298.
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Cancer Res.Home page
J.-G. Chen, C.-P. H. Yang, M. Cammer, and S. Band Horwitz
Gene Expression and Mitotic Exit Induced by Microtubule-Stabilizing Drugs
Cancer Res., November 15, 2003; 63(22): 7891 - 7899.
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J. Biol. Chem.Home page
S. Nagano, H. Li, H. Shimizu, C. Nishida, H. Ogura, P. R. O. de Montellano, and T. L. Poulos
Crystal Structures of Epothilone D-bound, Epothilone B-bound, and Substrate-free Forms of Cytochrome P450epoK
J. Biol. Chem., November 7, 2003; 278(45): 44886 - 44893.
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Ann OncolHome page
O. Smaletz, M. Galsky, H. I. Scher, A. DeLaCruz, S. F. Slovin, M. J. Morris, D. B. Solit, U. Davar, L. Schwartz, and W. K. Kelly
Pilot study of epothilone B analog (BMS-247550) and estramustine phosphate in patients with progressive metastatic prostate cancer following castration
Ann. Onc., October 1, 2003; 14(10): 1518 - 1524.
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Cancer Res.Home page
K. Kamath and M. A. Jordan
Suppression of Microtubule Dynamics by Epothilone B Is Associated with Mitotic Arrest
Cancer Res., September 15, 2003; 63(18): 6026 - 6031.
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Clin. Cancer Res.Home page
K. Pietras, M. Stumm, M. Hubert, E. Buchdunger, K. Rubin, C.-H. Heldin, P. McSheehy, M. Wartmann, and A. Ostman
STI571 Enhances the Therapeutic Index of Epothilone B by a Tumor-selective Increase of Drug Uptake
Clin. Cancer Res., September 1, 2003; 9(10): 3779 - 3787.
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T. L. Tinley, D. A. Randall-Hlubek, R. M. Leal, E. M. Jackson, J. W. Cessac, J. C. Quada Jr., T. K. Hemscheidt, and S. L. Mooberry
Taccalonolides E and A: Plant-derived Steroids with Microtubule-stabilizing Activity
Cancer Res., June 15, 2003; 63(12): 3211 - 3220.
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JCOHome page
J. Abraham, M. Agrawal, S. Bakke, A. Rutt, M. Edgerly, F. M. Balis, B. Widemann, L. Davis, B. Damle, D. Sonnichsen, et al.
Phase I Trial and Pharmacokinetic Study of BMS-247550, an Epothilone B Analog, Administered Intravenously on a Daily Schedule for Five Days
J. Clin. Oncol., May 1, 2003; 21(9): 1866 - 1873.
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J. F. Diaz, I. Barasoain, and J. M. Andreu
Fast Kinetics of Taxol Binding to Microtubules. EFFECTS OF SOLUTION VARIABLES AND MICROTUBULE-ASSOCIATED PROTEINS
J. Biol. Chem., February 28, 2003; 278(10): 8407 - 8419.
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S. Wittmann, P. Bali, S. Donapaty, R. Nimmanapalli, F. Guo, H. Yamaguchi, M. Huang, R. Jove, H. G. Wang, and K. Bhalla
Flavopiridol Down-Regulates Antiapoptotic Proteins and Sensitizes Human Breast Cancer Cells to Epothilone B-induced Apoptosis
Cancer Res., January 1, 2003; 63(1): 93 - 99.
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B. Julien and S. Shah
Heterologous Expression of Epothilone Biosynthetic Genes in Myxococcus xanthus
Antimicrob. Agents Chemother., September 1, 2002; 46(9): 2772 - 2778.
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Y.-H. Ling, J.-D. Jiang, J. F. Holland, and R. Perez-Soler
Arsenic Trioxide Produces Polymerization of Microtubules and Mitotic Arrest before Apoptosis in Human Tumor Cell Lines
Mol. Pharmacol., September 1, 2002; 62(3): 529 - 538.
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L. E. Broker, C. Huisman, C. G. Ferreira, J. A. Rodriguez, F. A. E. Kruyt, and G. Giaccone
Late Activation of Apoptotic Pathways Plays a Negligible Role in Mediating the Cytotoxic Effects of Discodermolide and Epothilone B in Non-Small Cell Lung Cancer Cells
Cancer Res., July 15, 2002; 62(14): 4081 - 4088.
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H. M. McDaid, S. Mani, H.-J. Shen, F. Muggia, D. Sonnichsen, and S. B. Horwitz
Validation of the Pharmacodynamics of BMS-247550, an Analogue of Epothilone B, during a Phase I Clinical Study
Clin. Cancer Res., July 1, 2002; 8(7): 2035 - 2043.
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T. Beckers, T. Reissmann, M. Schmidt, A. M. Burger, H. H. Fiebig, U. Vanhoefer, H. Pongratz, H. Hufsky, J. Hockemeyer, M. Frieser, et al.
2-Aroylindoles, a Novel Class of Potent, Orally Active Small Molecule Tubulin Inhibitors
Cancer Res., June 1, 2002; 62(11): 3113 - 3119.
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K. A. Hood, L. M. West, B. Rouwe, P. T. Northcote, M. V. Berridge, St. J. Wakefield, and J. H. Miller
Peloruside A, a Novel Antimitotic Agent with Paclitaxel-like Microtubule- stabilizing Activity
Cancer Res., June 1, 2002; 62(12): 3356 - 3360.
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J.-G. Chen and S. B. Horwitz
Differential Mitotic Responses to Microtubule-stabilizing and -destabilizing Drugs
Cancer Res., April 1, 2002; 62(7): 1935 - 1938.
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H. Yamaguchi, S. R. Paranawithana, M. W. Lee, Z. Huang, K. N. Bhalla, and H.-G. Wang
Epothilone B Analogue (BMS-247550)-mediated Cytotoxicity through Induction of Bax Conformational Change in Human Breast Cancer Cells
Cancer Res., January 1, 2002; 62(2): 466 - 471.
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Molecular Cancer TherapeuticsHome page
L. He, C.-P. Huang Yang, and S. B. Horwitz
Mutations in {beta}-Tubulin Map to Domains Involved in Regulation of Microtubule Stability in Epothilone- resistant Cell Lines
Mol. Cancer Ther., November 1, 2001; 1(1): 3 - 10.
[Abstract] [Full Text] [PDF]


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Proc. Natl. Acad. Sci. USAHome page
R. B. Lichtner, A. Rotgeri, T. Bunte, B. Buchmann, J. Hoffmann, W. Schwede, W. Skuballa, and U. Klar
Subcellular distribution of epothilones in human tumor cells
PNAS, September 13, 2001; (2001) 171023398.
[Abstract] [Full Text] [PDF]


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Proc. Natl. Acad. Sci. USAHome page
T.-C. Chou, O. A. O'Connor, W. P. Tong, Y. Guan, Z.-G. Zhang, S. J. Stachel, C. Lee, and S. J. Danishefsky
The synthesis, discovery, and development of a highly promising class of microtubule stabilization agents: Curative effects of desoxyepothilones B and F against human tumor xenografts in nude mice
PNAS, July 3, 2001; 98(14): 8113 - 8118.
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F. Y. F. Lee, R. Borzilleri, C. R. Fairchild, S.-H. Kim, B. H. Long, C. Reventos-Suarez, G. D. Vite, W. C. Rose, and R. A. Kramer
BMS-247550: A Novel Epothilone Analog with a Mode of Action Similar to Paclitaxel but Possessing Superior Antitumor Efficacy
Clin. Cancer Res., May 1, 2001; 7(5): 1429 - 1437.
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G. Bacher, B. Nickel, P. Emig, U. Vanhoefer, S. Seeber, A. Shandra, T. Klenner, and T. Beckers
D-24851, a Novel Synthetic Microtubule Inhibitor, Exerts Curative Antitumoral Activity in Vivo, Shows Efficacy toward Multidrug-resistant Tumor Cells, and Lacks Neurotoxicity
Cancer Res., January 1, 2001; 61(1): 392 - 399.
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M. Roberge, B. Cinel, H. J. Anderson, L. Lim, X. Jiang, L. Xu, C. M. Bigg, M. T. Kelly, and R. J. Andersen
Cell-based Screen for Antimitotic Agents and Identification of Analogues of Rhizoxin, Eleutherobin, and Paclitaxel in Natural Extracts
Cancer Res., September 1, 2000; 60(18): 5052 - 5058.
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L. A. Martello, H. M. McDaid, D. L. Regl, C.-P. H. Yang, D. Meng, T. R. R. Pettus, M. D. Kaufman, H. Arimoto, S. J. Danishefsky, A. B. Smith III, et al.
Taxol and Discodermolide Represent a Synergistic Drug Combination in Human Carcinoma Cell Lines
Clin. Cancer Res., May 1, 2000; 6(5): 1978 - 1987.
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C. Combeau, J. Provost, F. Lancelin, Y. Tournoux, F. Prod'homme, F. Herman, F. Lavelle, J. Leboul, and M. Vuilhorgne
RPR112378 and RPR115781: Two Representatives of a New Family of Microtubule Assembly Inhibitors
Mol. Pharmacol., March 1, 2000; 57(3): 553 - 563.
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JNCI J Natl Cancer InstHome page
L. M. Leoni, E. Hamel, D. Genini, H. Shih, C. J. Carrera, H. B. Cottam, and D. A. Carson
Indanocine, a Microtubule-Binding Indanone and a Selective Inducer of Apoptosis in Multidrug-Resistant Cancer Cells
J Natl Cancer Inst, February 2, 2000; 92(3): 217 - 224.
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ScienceHome page
L. Tang, S. Shah, L. Chung, J. Carney, L. Katz, C. Khosla, and B. Julien
Cloning and Heterologous Expression of the Epothilone Gene Cluster
Science, January 28, 2000; 287(5453): 640 - 642.
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B. Silakowski, H. U. Schairer, H. Ehret, B. Kunze, S. Weinig, G. Nordsiek, P. Brandt, H. Blocker, G. Hofle, S. Beyer, et al.
New Lessons for Combinatorial Biosynthesis from Myxobacteria. THE MYXOTHIAZOL BIOSYNTHETIC GENE CLUSTER OF Stigmatella aurantiaca DW4/3-1
J. Biol. Chem., December 24, 1999; 274(52): 37391 - 37399.
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I. Ojima, S. Chakravarty, T. Inoue, S. Lin, L. He, S. B. Horwitz, S. D. Kuduk, and S. J. Danishefsky
A common pharmacophore for cytotoxic natural products that stabilize microtubules
PNAS, April 13, 1999; 96(8): 4256 - 4261.
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C. Dumontet and B. I. Sikic
Mechanisms of Action of and Resistance to Antitubulin Agents: Microtubule Dynamics, Drug Transport, and Cell Death
J. Clin. Oncol., March 1, 1999; 17(3): 1061 - 1061.
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S. L. Mooberry, G. Tien, A. H. Hernandez, A. Plubrukarn, and B. S. Davidson
Laulimalide and Isolaulimalide, New Paclitaxel-Like Microtubule-Stabilizing Agents
Cancer Res., February 1, 1999; 59(3): 653 - 660.
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T.-C. Chou, X.-G. Zhang, C. R. Harris, S. D. Kuduk, A. Balog, K. A. Savin, J. R. Bertino, and S. J. Danishefsky
Desoxyepothilone B is curative against human tumor xenografts that are refractory to paclitaxel
PNAS, December 22, 1998; 95(26): 15798 - 15802.
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Proc. Natl. Acad. Sci. USAHome page
S. C. Sinha, C. F. Barbas III, and R. A. Lerner
The antibody catalysis route to the total synthesis of epothilones
PNAS, December 8, 1998; 95(25): 14603 - 14608.
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T.-C. Chou, X.-G. Zhang, A. Balog, D.-S. Su, D. Meng, K. Savin, J. R. Bertino, and S. J. Danishefsky
Desoxyepothilone B: An efficacious microtubule-targeted antitumor agent with a promising in vivo profile relative to epothilone B
PNAS, August 4, 1998; 95(16): 9642 - 9647.
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Proc. Natl. Acad. Sci. USAHome page
P. J. Moos and F. A. Fitzpatrick
Taxane-mediated gene induction is independent of microtubule stabilization: Induction of transcription regulators and enzymes that modulate inflammation and apoptosis
PNAS, March 31, 1998; 95(7): 3896 - 3901.
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Proc. Natl. Acad. Sci. USAHome page
M. M. Moasser, L. Sepp-Lorenzino, N. E. Kohl, A. Oliff, A. Balog, D.-S. Su, S. J. Danishefsky, and N. Rosen
Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones
PNAS, February 17, 1998; 95(4): 1369 - 1374.
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