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SKLB060 Reversibly Binds to Colchicine Site of Tubulin and Possesses Efficacy in Multidrug-Resistant Cell Lines

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Possible binding site for paclitaxel at microtubule pores

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Taxanes with high potency inducing tubulin assembly overcome tumoural cell resistances

Matesanz, R., Trigili, C., Rodríguez‐Salarichs, J., Zanardi, I., Pera, B., Nogales, A., Fang, W., Jiménez‐Barbero, J., Canales, Á., Barasoaı́n, I., et al. (2014) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2014.05.048 · Cited by 36 · see citing works

Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules

Marco, J. A., García-Pla, J., Cardá, M., Murga, J., Falomir, E., Trigili, C., Notararigo, S., Díaz, J. F., & Barasoaı́n, I. (2011) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2011.02.011 · Cited by 35 · see citing works

Synthesis and Biological Evaluation of Colchicine B-Ring Analogues Tethered with Halogenated Benzyl Moieties

Cosentino, L., Redondo‐Horcajo, M., Zhao, Y., Santos, A. R., Chowdury, K. F., Vinader, V. M., Abdallah, Q., Abdel-Rahman, H. M., Chabert, J. F. D., Shnyder, S. D., et al. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm301151t · Cited by 34 · see citing works

The Assembly-Inducing Laulimalide/Peloruside A Binding Site on Tubulin: Molecular Modeling and Biochemical Studies with [3H]Peloruside A

Nguyen, T. L., Xu, X., Gussio, R., Ghosh, A. K., & Hamel, E. (2010) · Journal of Chemical Information and Modeling · doi:10.1021/ci1002894 · Cited by 34 · see citing works

Theoretical analysis of bacterial efflux pumps inhibitors: Strategies in-search of competent molecules and develop next

Ghosh, A. K., Roymahapatra, G., Paul, D., & Mandal, S. M. (2020) · Computational Biology and Chemistry · doi:10.1016/j.compbiolchem.2020.107275 · Cited by 33 · see citing works

Total Synthesis and Biological Evaluation of a Series of Macrocyclic Hybrids and Analogues of the Antimitotic Natural Products Dictyostatin, Discodermolide, and Taxol

Paterson, I., Naylor, G. J., Gardner, N. M., Guzmán, E. A., & Wright, A. E. (2010) · Chemistry - An Asian Journal · doi:10.1002/asia.201000541 · Cited by 32 · see citing works

Modulation of Microtubule Interprotofilament Interactions by Modified Taxanes

Matesanz, R., Rodríguez‐Salarichs, J., Pera, B., Canales, Á., Andreu, J. M., Jiménez‐Barbero, J., Bras, W., Nogales, A., Fang, W., & Díaz, J. F. (2011) · Biophysical Journal · doi:10.1016/j.bpj.2011.11.005 · Cited by 32 · see citing works

The Natural Compound Withaferin A Covalently Binds to Cys239 of β-Tubulin to Promote Tubulin Degradation

Yang, J., Yan, W., Li, Y., Niu, L., Ye, H., & Chen, L. (2019) · Molecular Pharmacology · doi:10.1124/mol.119.117812 · Cited by 31 · see citing works

Zampanolide, a Microtubule-Stabilizing Agent, Is Active in Resistant Cancer Cells and Inhibits Cell Migration

Field, J., Northcote, P. T., Paterson, I., Altmann, K., Díaz, J. F., & Miller, J. H. (2017) · International Journal of Molecular Sciences · doi:10.3390/ijms18050971 · Cited by 29 · see citing works

Molecular Recognition of Epothilones by Microtubules and Tubulin Dimers Revealed by Biochemical and NMR Approaches

Canales, Á., Nieto, L., Rodríguez‐Salarichs, J., Sánchez‐Murcia, P. A., Coderch, C., Cortés-Cabrera, Á., Paterson, I., Carlomagno, T., Gago, F., Andreu, J. M., et al. (2014) · ACS Chemical Biology · doi:10.1021/cb400673h · Cited by 28 · see citing works

Simulations of Tubulin Sheet Polymers as Possible Structural Intermediates in Microtubule Assembly

Wu, Z., Wang, H., Mu, W., Ouyang, Z., Nogales, E., & Xing, J. (2009) · PLoS ONE · doi:10.1371/journal.pone.0007291 · Cited by 28 · see citing works

Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands

Balaguer, F. D. A., Mühlethaler, T., Estévez‐Gallego, J., Calvo, E., Giménez-Abián, J. F., Risinger, A. L., Sorensen, E. J., Vanderwal, C. D., Altmann, K., Mooberry, S. L., et al. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20061392 · Cited by 28 · see citing works

Fluorescent Taxoid Probes for Microtubule Research

Barasoaı́n, I., Díaz, J. F., & Andreu, J. M. (2010) · Methods in cell biology · doi:10.1016/s0091-679x(10)95019-x · Cited by 27 · see citing works

Molecular Recognition of Peloruside A by Microtubules. The C24 Primary Alcohol is Essential for Biological Activity

Pera, B., Razzak, M., Trigili, C., Pineda, O., Canales, Á., Buey, R. M., Jiménez‐Barbero, J., Northcote, P. T., Paterson, I., Barasoaı́n, I., et al. (2010) · ChemBioChem · doi:10.1002/cbic.201000294 · Cited by 27 · see citing works

The Tubulin‐Bound Structure of the Antimitotic Drug Tubulysin

Kubíček, K., Grimm, S. K., Orts, J., Sasse, F., & Carlomagno, T. (2010) · Angewandte Chemie International Edition · doi:10.1002/anie.200906828 · Cited by 27 · see citing works

Emerging targets and new small molecule therapies in Parkinson’s disease treatment

Zhang, H., Tong, R., Bai, L., Shi, J., & Ouyang, L. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.02.030 · Cited by 26 · see citing works

Multiwell Raman plate reader for high-throughput biochemical screening

Kawagoe, H., Ando, J., Asanuma, M., Dodo, K., Miyano, T., Ueda, H., Sodeoka, M., & Fujita, K. (2021) · Scientific Reports · doi:10.1038/s41598-021-95139-8 · Cited by 26 · see citing works

Microtubule stabilising agents for cancer chemotherapy

Zhao, Y., Fang, W., & Pors, K. (2009) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543770902775713 · Cited by 25 · see citing works

Probing the Pore Drug Binding Site of Microtubules with Fluorescent Taxanes: Evidence of Two Binding Poses

Barasoaı́n, I., García-Carril, A. M., Matesanz, R., Maccari, G., Trigili, C., Mori, M., Shi, J.-Z., Fang, W., Andreu, J. M., Botta, M., et al. (2010) · Chemistry & Biology · doi:10.1016/j.chembiol.2010.02.006 · Cited by 25 · see citing works

High affinity and covalent-binding microtubule stabilizing agents show activity in chemotherapy-resistant acute myeloid leukemia cells

Pera, B., Calvo-Vidal, M. N., Ambati, S. R., Jordi, M., Kahn, A. R., Díaz, J. F., Fang, W., Altmann, K., Cerchietti, L. C. A., & Moore, M. A. S. (2015) · Cancer Letters · doi:10.1016/j.canlet.2015.07.038 · Cited by 24 · see citing works

Drugs That Changed Society: Microtubule-Targeting Agents Belonging to Taxanoids, Macrolides and Non-Ribosomal Peptides

Christensen, S. B. (2022) · Molecules · doi:10.3390/molecules27175648 · Cited by 24 · see citing works

Synthesis and biological evaluation of new oxadiazoline-substituted naphthalenyl acetates as anticancer agents

Chaaban, I., Khawass, E. S. M. E., Razik, H. A. A. E., Salamouni, N. S. E., Redondo‐Horcajo, M., Barasoaı́n, I., Díaz, J. F., Yli‐Kauhaluoma, J. T., & Moreira, V. M. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.10.015 · Cited by 24 · see citing works

Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites

Field, J. J., Pera, B., Estévez‐Gallego, J., Calvo, E., Rodríguez‐Salarichs, J., Sáez-Calvo, G., Zuwerra, D., Jordi, M., Andreu, J. M., Prota, A. E., et al. (2017) · Journal of Natural Products · doi:10.1021/acs.jnatprod.7b00704 · Cited by 22 · see citing works

15-Deoxi-Δ12,14-prostaglandin J2 is a tubulin-binding agent that destabilizes microtubules and induces mitotic arrest

Cocca, C., Navarro‐Dorado, J., Calvo, E., López, J. A., Santos, Á., & Pérez‐Castillo, A. (2009) · Biochemical Pharmacology · doi:10.1016/j.bcp.2009.06.100 · Cited by 21 · see citing works

Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ

Risinger, A. L., Li, J., Du, L., Benavides, R., Robles, A. J., Cichewicz, R. H., Kuhn, J. G., & Mooberry, S. L. (2017) · Journal of Natural Products · doi:10.1021/acs.jnatprod.6b00944 · Cited by 21 · see citing works

Discovery of a Series of Hydroxamic Acid-Based Microtubule Destabilizing Agents with Potent Antitumor Activity

Yang, L., Zhang, W., Qiu, Q., Su, Z., Tang, M., Bai, P., Si, W., Zhu, Z., Liu, Y., Yang, J., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01451 · Cited by 21 · see citing works

Modeling the Yew Tree Tubulin and a Comparison of its Interaction with Paclitaxel to Human Tubulin

Tuszyński, J. A., Craddock, T. J. A., Mane, J. Y., Barakat, K., Tseng, C., Gajewski, M. M., Winter, P., Alisaraie, L., Patterson, J., Carpenter, E. J., et al. (2012) · Pharmaceutical Research · doi:10.1007/s11095-012-0829-y · Cited by 20 · see citing works

Synthesis and biological evaluation of truncated α-tubulin-binding pironetin analogues lacking alkyl pendants in the side chain or the dihydropyrone ring

Paños, J., Díaz‐Oltra, S., Sánchez‐Peris, M., García-Pla, J., Murga, J., Falomir, E., Cardá, M., Redondo‐Horcajo, M., Díaz, J. F., Barasoaı́n, I., et al. (2013) · Organic & Biomolecular Chemistry · doi:10.1039/c3ob40854j · Cited by 20 · see citing works

Cyclostreptin Derivatives Specifically Target Cellular Tubulin and Further Map the Paclitaxel Site

Calvo, E., Barasoaı́n, I., Matesanz, R., Pera, B., Camafeita, E., Pineda, O., Hamel, E., Vanderwal, C. D., Andreu, J. M., López, J. A., et al. (2011) · Biochemistry · doi:10.1021/bi201380p · Cited by 20 · see citing works

Highly Stereoselective Total Synthesis of (+)‐9‐epi‐Dictyostatin and (–)‐12,13‐Bis‐epi‐dictyostatin

Zanato, C., Pignataro, L., Ambrosi, A., Hao, Z.-Y., Trigili, C., Díaz, J. F., Barasoaı́n, I., & Gennari, C. (2011) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201100244 · Cited by 18 · see citing works

Characterization of the Covalent Binding of N-Phenyl-N′-(2-chloroethyl)ureas to β-Tubulin: Importance of Glu198 in Microtubule Stability

Fortin, S., Bouchon, B., Chambon, C., Lacroix, J., Moreau, E., Chezal, J., Degoul, F., & Gaudreault, R. C. (2010) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.110.171082 · Cited by 18 · see citing works

The Tubulin Binding Mode of Microtubule Stabilizing Agents Studied by Electron Crystallography

Nettles, J. H., & Downing, K. H. (2008) · Topics in current chemistry · doi:10.1007/128_2008_24 · Cited by 16 · see citing works

Cyclostreptin and Microtubules: Is a Low‐Affinity Binding Site Required?

Prussia, A. J., Yang, Y., Geballe, M. T., & Snyder, J. P. (2009) · ChemBioChem · doi:10.1002/cbic.200900538 · Cited by 16 · see citing works

PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin

Lucena‐Agell, D., Guillén, M. J., Matesanz, R., Álvarez‐Bernad, B., Hortigüela, R., Avilés, P., Martínez, M., Santamaria-Nuñez, G., Contreras, J., Plaza-Menacho, I., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01775 · Cited by 15 · see citing works

The Interaction of Microtubules with Stabilizers Characterized at Biochemical and Structural Levels

Díaz, J. F., Andreu, J. M., & Jiménez‐Barbero, J. (2008) · Topics in current chemistry · doi:10.1007/128_2008_12 · Cited by 15 · see citing works

An Overview of Compounds That Interact with Tubulin and Their Effects on Microtubule Assembly

Hamel, E. (2009) · Humana Press eBooks · doi:10.1007/978-1-59745-336-3_1 · Cited by 15 · see citing works

Designing and Testing of Novel Taxanes to Probe the Highly Complex Mechanisms by Which Taxanes Bind to Microtubules and Cause Cytotoxicity to Cancer Cells

George, M. S., Ayoub, A. T., Banerjee, A. K., Churchill, C. D. M., Winter, P., Kłobukowski, M., Cass, C. E., Ludueña, R. F., Tuszyński, J. A., & Damaraju, S. (2015) · PLoS ONE · doi:10.1371/journal.pone.0129168 · Cited by 15 · see citing works

Unravelling the covalent binding of zampanolide and taccalonolide AJ to a minimalist representation of a human microtubule

Sánchez‐Murcia, P. A., Mills, A., Cortés-Cabrera, Á., & Gago, F. (2019) · Journal of Computer-Aided Molecular Design · doi:10.1007/s10822-019-00208-w · Cited by 15 · see citing works

The microtubule-pore gatekeeper

Snyder, J. P. (2007) · Nature Chemical Biology · doi:10.1038/nchembio0207-81 · Cited by 14 · see citing works

Asymmetric and Highly Stereoselective Synthesis of the DEF-Ring Moiety of (−)-FR182877 and Its Derivative Inducing Mitotic Arrest

Kobayakawa, Y., Mori, Y., Okajima, H., Terada, Y., & Nakada, M. (2012) · Organic Letters · doi:10.1021/ol300615w · Cited by 14 · see citing works

Interaction of a Cyclostreptin Analogue with the Microtubule Taxoid Site: The Covalent Reaction Rapidly Follows Binding

Bai, R., Vanderwal, C. D., Díaz, J. F., & Hamel, E. (2008) · Journal of Natural Products · doi:10.1021/np800056m · Cited by 14 · see citing works

Making Epothilones Fluoresce: Design, Synthesis, and Biological Characterization of a Fluorescent N12‐Aza‐Epothilone (Azathilone)

Gertsch, J., Feyen, F., Bützberger, A., Gerber, B., Pfeiffer, B., & Altmann, K. (2009) · ChemBioChem · doi:10.1002/cbic.200900376 · Cited by 13 · see citing works

Microtubule Targeting Agents in Cancer Therapy: Elucidating the Underlying Molecular Mechanisms

Hasanpourghadi, M., Pandurangan, A. K., & Mustafa, M. R. (2017) · Springer eBooks · doi:10.1007/978-3-319-53082-6_2 · Cited by 12 · see citing works

Cyclostreptin Derivatives Specifically Target Cellular Tubulin and Further Map the Paclitaxel Site

Calvo, E., Barasoaı́n, I., Matesanz, R., Pera, B., Camafeita, E., Pineda, O., Hamel, E., Vanderwal, C. D., Andreu, J. M., López, J. A., et al. (2011) · Biochemistry · doi:10.1021/bi201380p · Cited by 20 · see citing works

The microtubule-pore gatekeeper

Snyder, J. P. (2007) · Nature Chemical Biology · doi:10.1038/nchembio0207-81 · Cited by 14 · see citing works

Cyclostreptin (FR182877), an Antitumor Tubulin-Polymerizing Agent Deficient in Enhancing Tubulin Assembly Despite Its High Affinity for the Taxoid Site

Edler, M., Buey, R. M., Gussio, R., Marcus, A. I., Vanderwal, C. D., Sorensen, E. J., Díaz, J. F., Giannakakou, P., & Hamel, E. (2005) · Biochemistry · doi:10.1021/bi050660m · Cited by 64 · see citing works

In this issue

(2007) · Nature Chemical Biology · doi:10.1038/nchembio0207-v

Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands

Balaguer, F. D. A., Mühlethaler, T., Estévez‐Gallego, J., Calvo, E., Giménez-Abián, J. F., Risinger, A. L., Sorensen, E. J., Vanderwal, C. D., Altmann, K., Mooberry, S. L., et al. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20061392 · Cited by 28 · see citing works