Enzyme Inhibitors May Lead to Cancer Drug

The results were presented at the International Conference on Molecular Cancer Targets in Frankfurt (German).

LPAAT-beta is highly expressed in cancers of the lung, ovary, bladder, and cervix, while it is minimally expressed in most normal tissues. Scientists believe that cells become more tumorigenic when the enzyme is overexpressed because PPAAT-beta produces phosphatidic acid (PA), an essential cofactor for two signaling molecules, RAF and AKT, both important to cancer cell survival. The AKT signaling pathway is active in 70% of tumors and is considered to be a critical pathway with considerable potential for cancer-specific, drug-mediated intervention.

The scientists, from Cell Therapeutics, Inc. (CTI, Seattle, WA, USA; ), have found that inhibiting LPAAT-beta kills cancer cells. They are developing drugs to inhibit LPAAT-beta and have shown that these compounds induce apoptosis in a wide variety of tumor cell lines and delay tumor growth in animal models of colorectal and lung cancer without producing significant toxicities. "The experiments in animal models show that the small molecule LPAAT-beta inhibitors can effectively kill tumor cells without having pronounced effects on normal cells,” said Jack W. Singer, M.D., research program chairman of CTI.




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Cell Therapeutics, Inc.