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Published in final edited form as: Pharmacol Ther. 2017 Mar 27;178:92–108. doi: 10.1016/j.pharmthera.2017.03.013
Abstract
The tumor suppressor p53 is one of the most important proteins for protection of genomic stability and cancer prevention. Cancers often inactivate it by either mutating its gene or disabling its function. Thus, activating p53 becomes an attractive approach for the development of molecule-based anti-cancer therapy. The past decade and half have witnessed tremendous progress in this area. This essay offers readers with a grand review on this progress with updated information about small molecule activators of p53 either still at bench work or in clinical trials.
Keywords: p53, small molecules, MDM2, MDMX, drug discovery, Inauhzin
Introduction
For many decades, cancer therapy had relied entirely on chemotherapeutic agents in the forms of antimetabolites, alkylating agents, various alkaloids, cytotoxic antibiotics, and other chemicals that target rapidly proliferating cells through different mechanisms such as topoisomerase inhibition, DNA intercalation, and microtubule polymerization (Chabner & Roberts, 2005). With no other options available, chemotherapy, as a consequence of its inherent cytotox
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