2. Academic Validation
  3. Tubulin binding, protein-bound conformation in solution, and antimitotic cellular profiling of noscapine and its derivatives

Tubulin binding, protein-bound conformation in solution, and antimitotic cellular profiling of noscapine and its derivatives

  • J Med Chem. 2012 Mar 8;55(5):1920-5. doi: 10.1021/jm200848t.
Youssef L Bennani 1,  Wenxin Gu,  Angeles Canales,  Fernando J Díaz,  Brenda K Eustace,  Russell R Hoover,  Jesus Jiménez-Barbero,  Azin Nezami,  Tiansheng Wang
Affiliations

Affiliation

  • 1 Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge Massachusetts 02139, USA. youssef_Bennani@vrtx.com
PMID: 22320354 DOI: 10.1021/jm200848t
Abstract

Noscapine and its 7-hydroxy and 7-amino derivatives were characterized for their binding to tubulin. A solution NMR structure of these compounds bound to tubulin shows that noscapine and its 7-aniline derivative do not compete for the same binding site nor does its small molecule crystal structure match its tubulin-bound conformation. These compounds were also tested for their antiproliferative effects on a panel hepatocellular carcinoma cell lines.

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