Understanding and Exploiting Natures Chemical Arsenal: The Past,Present and Future of Calicheamicin Research

Author(s): Jon S. Thorson, Eric L. Sievers, Joachim Ahlert, Erica Shepard, Ross E. Whitwam, Kenolisa C. Onwueme, Mark Ruppen.

Journal Name: Current Pharmaceutical Design

Volume 6 , Issue 18 , 2000


The enediyne antitumor antibiotics are appreciated for their novel molecular architecture, their remarkable biological activity and their fascinating mode of action and many have spawned considerable interest as anticancer agents in the pharmaceutical industry. Of equal importance to these astonishing properties, the enediynes also offer a distinct opportunity to study the unparalleled biosyntheses of their unique molecular scaffolds and what promises to be unprecedented modes of self-resistance to highly reactive natural products. Elucidation of these aspects should unveil novel mechanistic enzymology, and may provide access to the rational biosynthetic modification of enediyne structure for new drug leads, the construction of enediyne overproducing strains and eventually lead to an enediyne combinatorial biosynthesis program. This article strives to compile and present the critical research discoveries relevant to the clinically most promising enediyne, calicheamicin, from a historical perspective. Recent progress, particularly in the areas of biosynthesis, self-resistance, bio-engineering analogs and clinical studies are also highlighted.

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Article Details

Year: 2000
Page: [1841 - 1879]
Pages: 39
DOI: 10.2174/1381612003398564
Price: $58

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