ChemMedChem

Cover image for Vol. 12 Issue 10

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

October 26, 2010

VIP: Chemotherapeutic Evaluation of a Synthetic Tubulysin Analogue–Dendrimer Conjugate in C26 Tumor Bearing Mice

VIP: Chemotherapeutic Evaluation of a Synthetic Tubulysin Analogue–Dendrimer Conjugate in C26 Tumor Bearing MiceWilliam C. Floyd III, Gopal K. Datta, Shinichi Imamura, Heidi M. Kieler-Ferguson, Katherine Jerger, Andrew W. Patterson, Megan E. Fox, Francis C. Szoka,* Jean M. J. Fréchet,* and Jonathan A. Ellman*

The tubulysins are a family of natural products with interesting structural properties and exceedingly potent cytotoxicity, which is brought about by their inhibition of tubulin polymerization and subsequent induction of apoptosis. They have therefore been the subject of a broad scope of research efforts in synthesis, biosynthesis, structure–activity relationships, bioactivity, mode of action, and chemotherapeutic potential. Szoka, Fréchet, Ellman, and colleagues report the first application of polymeric drug delivery using synthetic tubulysin analogues, which overcome many of the liabilities of the naturally occurring tubulysins, including ease of synthesis and high stability. The application of this dendrimer conjugation technology has resulted in promising efficacy without toxicity in animal trials.

Received September 6, 2010; published online October 25, 2010, DOI: 10.1002/cmdc.201000377.

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