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3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin.
La Regina G, Bai R, Coluccia A, Famiglini V, Passacantilli S, Naccarato V, Ortar G, Mazzoccoli C, Ruggieri V, Agriesti F, Piccoli C, Tataranni T, Nalli M, Brancale A, Vultaggio S, Mercurio C, Varasi M, Saponaro C, Sergio S, Maffia M, Coluccia AML, Hamel E, Silvestri R. La Regina G, et al. Among authors: hamel e. ACS Med Chem Lett. 2017 Apr 26;8(5):521-526. doi: 10.1021/acsmedchemlett.7b00022. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523104 Free PMC article.
Identification of the cysteine residue of beta-tubulin alkylated by the antimitotic agent 2,4-dichlorobenzyl thiocyanate, facilitated by separation of the protein subunits of tubulin by hydrophobic column chromatography.
Bai RL, Lin CM, Nguyen NY, Liu TY, Hamel E. Bai RL, et al. Among authors: hamel e. Biochemistry. 1989 Jun 27;28(13):5606-12. doi: 10.1021/bi00439a040. Biochemistry. 1989. PMID: 2775724
Shown in previous studies to inhibit tubulin polymerization [Abraham, I., Dion, R. L., Duanmu, C., Gottesman, M. M., & Hamel, E. (1986) Proc. Natl. Acad. Sci. U.S.A. 83, 6839-6843] and to form a covalent bond preferentially with beta-tubulin [Bai, R., Duanmu, C. …
Shown in previous studies to inhibit tubulin polymerization [Abraham, I., Dion, R. L., Duanmu, C., Gottesman, M. M., & Hamel, …
Mechanism of action of the antimitotic drug 2,4-dichlorobenzyl thiocyanate: alkylation of sulfhydryl group(s) of beta-tubulin.
Bai R, Duanmu C, Hamel E. Bai R, et al. Among authors: hamel e. Biochim Biophys Acta. 1989 Jan 19;994(1):12-20. doi: 10.1016/0167-4838(89)90056-3. Biochim Biophys Acta. 1989. PMID: 2909252
The compound, 2,4-dichlorobenzyl thiocyanate (DCBT) was previously shown to cause mitotic arrest, disruption of intracellular microtubules, and inhibition of tubulin polymerization, with resistance to the drug conferred by a mutation in a beta-tubulin gene (Abraham, I., Dion, R.L …
The compound, 2,4-dichlorobenzyl thiocyanate (DCBT) was previously shown to cause mitotic arrest, disruption of intracellular microtubules, …
651 results