Inhibitors of Human Apurinic/apyrimidinic Endonuclease 1 (APE1), an Anticancer Drug Target
Lead Inventor: David Maloney (NCATS)
Ref. No.: E-094-2011/0
Abstract: APE1 is the primary mammalian enzyme responsible for the removal of abasic (AP sites) in DNA and functions as part of the base excision DNA repair pathway (BER). BER is instrumental in the repair of DNA damage caused by DNA alkylating agents (e.g. many cancer chemotherapeutics). APE1 has been shown to be overexpressed in cancer cells. It has been postulated that APE1 would be an attractive target in anti-cancer treatment paradigms; pre-clinical and clinical data confirm that APE1 is a valid anticancer drug target.
Publications:
Synthesis, Biological Evaluation, and Structure-Activity Relationships of a Novel Class of Apurinic/Apyrimidinic Endonuclease 1 Inhibitors • Journal of Medicinal Chemistry • April 12, 2012 • Probe Development Branch,
NCATS Chemical Genomics Center
Human AP Endonuclease 1 (APE1): From Mechanistic Insights to Druggable Target in Cancer • Cancer Treatment Reviews • August 2010 • Probe Development Branch, NCATS Chemical Genomics Center