The therapeutic potential of O6-alkylguanine DNA alkyltransferase inhibitors.

Journal article

Resistance to O(6-)alkylating agents can be overcome by depletion of the DNA repair protein, O(6)-alkylguanine DNA alkyltransferase. Inhibitors of this protein act as pseudosubstrates and, so far, O(6)-benzylguanine and lomeguatrib have been tested in clinical trials. Inherently non-toxic, optimum doses for protein depletion have been established for both agents. Myelosuppression of alkylating agents is significantly enhanced when used in combination with these agents, necessitating significa...

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Authors: Khan, O; Middleton, MR

• Publication status: Published
• Journal: Expert opinion on investigational drugs
• Volume: 16
• Issue: 10
• Pages: 1573-1584
• Publication date: 2007-10-01
• DOI: 10.1517/13543784.16.10.1573
• EISSN: 1744-7658
• ISSN: 1354-3784
• Language: English
• Keywords: O(6)-Methylguanine-DNA Methyltransferase; Clinical Trials as Topic; Humans; Antineoplastic Agents, Alkylating; Neoplasms; Animals