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Modulation of taxane binding to tubulin curved and straight conformations by systematic 3'N modification provides for improved microtubule binding, persistent cytotoxicity and in vivo potency.
Ma Y, Josa-Prado F, Essif JN, Liu S, Li S, Lucena-Agell D, Chan PY, Goossens K, Hortigüela R, Matesanz R, Wang Y, Gago F, Wang H, Risinger A, Diaz JF, Fang WS. Ma Y, et al. Among authors: fang ws. Eur J Med Chem. 2023 Nov 5;259:115668. doi: 10.1016/j.ejmech.2023.115668. Epub 2023 Jul 19. Eur J Med Chem. 2023. PMID: 37490800
Structural insight into the stabilization of microtubules by taxanes.
Prota AE, Lucena-Agell D, Ma Y, Estevez-Gallego J, Li S, Bargsten K, Josa-Prado F, Altmann KH, Gaillard N, Kamimura S, Mühlethaler T, Gago F, Oliva MA, Steinmetz MO, Fang WS, Díaz JF. Prota AE, et al. Among authors: fang ws. Elife. 2023 Mar 6;12:e84791. doi: 10.7554/eLife.84791. Elife. 2023. PMID: 36876916 Free PMC article.
Targeting the tubulin C-terminal tail by charged small molecules.
Li S, Mori M, Yang M, Elfazazi S, Hortigüela R, Chan P, Feng X, Risinger A, Yang Z, Oliva MÁ, Fernando Díaz J, Fang WS. Li S, et al. Among authors: fang ws. Org Biomol Chem. 2022 Dec 21;21(1):153-162. doi: 10.1039/d2ob01910h. Org Biomol Chem. 2022. PMID: 36472095
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: fang ws. Nat Mater. 2020 Mar;19(3):355-365. doi: 10.1038/s41563-019-0546-6. Epub 2019 Dec 9. Nat Mater. 2020. PMID: 31819210
69 results