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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Targeting Heme for the Identification of Cytotoxic Agents

Author(s): Shiming Zhang, Hui Chen, Jessica Webster and Glenn S. Gerhard

Volume 13 , Issue 3 , 2013

Page: [515 - 522] Pages: 8

DOI: 10.2174/1871520611313030014

Price: $65


Certain tumor types have an increased capacity for heme synthesis, which serves as the basis for photodynamic therapy. Heme also serves as the target for the anti-malaria drug artemisinin, which has also been used as an anti-cancer drug. We developed a highthroughput screening assay to identify heme interacting (HI) compounds, which included imidazole, pyridine, carbonitrile, isocyanide, and quinoline core structures that are known to interact with heme or hemin. The cytotoxicity of several of the compounds towards human leukemia cell lines could be modulated by increasing or decreasing heme synthesis. Spectral analysis indicated that distinct molecular interactions occurred with heme, suggesting that HI compounds appear to target heme with exquisite specificity. These studies suggest that heme may serve as a novel therapeutic target for cancer drug discovery.

Keywords: Heme, Target, Cancer, High-throughput screen, Cytotoxicity

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