DNA damage response and repair pathways are at the forefront of molecularly-targeted therapeutic strategies, as tumor-induced defects in DNA repair or checkpoint signaling can be exploited by selective targeting of other repair pathways. This is exemplified by successful targeting of PARP1/2, Chk1/Wee1, and ATM/ATR, as well as additional drug development efforts focused on DNA repair. This symposium highlights resurgent interests in selective targeting of these survival pathways, and how these efforts may be exploited to augment current cancer therapy, topics which are timely and of significant impact in the fields of cancer pharmacology, drug discovery and drug development.