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Tumor O(6)-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib.

Abstract:

PURPOSE: A major mechanism of resistance to chlorethylnitrosureas and methylating agents involves the DNA repair protein O(6)-methylguanine-DNA methyltransferase (MGMT). We sought to determine the dose of oral 6-(4-bromo-2-thienyl) methoxy purin-2-amine (lomeguatrib), a pseudosubstrate inactivator of MGMT, required to render active protein undetectable 12 hours after dosing in prostate, primary central nervous system (CNS), and colorectal cancer patients. EXPERIMENTAL DESIGN: Lomeguatrib was ...

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Publication status:
Published

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Journal:
Clinical cancer research : an official journal of the American Association for Cancer Research
Volume:
16
Issue:
2
Pages:
743-749
Publication date:
2010-01-01
DOI:
EISSN:
1557-3265
ISSN:
1078-0432
Source identifiers:
120091

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