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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: diaz jf. 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
Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites.
Buey RM, Calvo E, Barasoain I, Pineda O, Edler MC, Matesanz R, Cerezo G, Vanderwal CD, Day BW, Sorensen EJ, López JA, Andreu JM, Hamel E, Díaz JF. Buey RM, et al. Among authors: diaz jf. Nat Chem Biol. 2007 Feb;3(2):117-25. doi: 10.1038/nchembio853. Epub 2007 Jan 7. Nat Chem Biol. 2007. PMID: 17206139 Free article.
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.
La Regina G, Edler MC, Brancale A, Kandil S, Coluccia A, Piscitelli F, Hamel E, De Martino G, Matesanz R, Díaz JF, Scovassi AI, Prosperi E, Lavecchia A, Novellino E, Artico M, Silvestri R. La Regina G, et al. Among authors: diaz jf. J Med Chem. 2007 Jun 14;50(12):2865-74. doi: 10.1021/jm061479u. Epub 2007 May 12. J Med Chem. 2007. PMID: 17497841
211 results