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Zampanolide, a potent new microtubule-stabilizing agent, covalently reacts with the taxane luminal site in tubulin α,β-heterodimers and microtubules.
Field JJ, Pera B, Calvo E, Canales A, Zurwerra D, Trigili C, Rodríguez-Salarichs J, Matesanz R, Kanakkanthara A, Wakefield SJ, Singh AJ, Jiménez-Barbero J, Northcote P, Miller JH, López JA, Hamel E, Barasoain I, Altmann KH, Díaz JF. Field JJ, et al. Among authors: altmann kh. Chem Biol. 2012 Jun 22;19(6):686-98. doi: 10.1016/j.chembiol.2012.05.008. Chem Biol. 2012. PMID: 22726683 Free PMC article.
Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands.
Balaguer FA, Mühlethaler T, Estévez-Gallego J, Calvo E, Giménez-Abián JF, Risinger AL, Sorensen EJ, Vanderwal CD, Altmann KH, Mooberry SL, Steinmetz MO, Oliva MÁ, Prota AE, Díaz JF. Balaguer FA, et al. Among authors: altmann kh. Int J Mol Sci. 2019 Mar 20;20(6):1392. doi: 10.3390/ijms20061392. Int J Mol Sci. 2019. PMID: 30897704 Free PMC article.
Taxanes convert regions of perturbed microtubule growth into rescue sites.
Rai A, Liu T, Glauser S, Katrukha EA, Estévez-Gallego J, Rodríguez-García R, Fang WS, Díaz JF, Steinmetz MO, Altmann KH, Kapitein LC, Moores CA, Akhmanova A. Rai A, et al. Among authors: altmann kh. Nat Mater. 2020 Mar;19(3):355-365. doi: 10.1038/s41563-019-0546-6. Epub 2019 Dec 9. Nat Mater. 2020. PMID: 31819210
174 results