DNA damage response (DDR) is a complicated interactional pathway. Defects that occur in
subordinate pathways of the DDR pathway can lead to genomic instability and cancer susceptibility.
Abnormal expression of some proteins in DDR, especially in the DNA repair pathway, are associated
with the subsistence and resistance of cancer cells. Therefore, the development of small molecule inhibitors
targeting the chief proteins in the DDR pathway is an effective strategy for cancer therapy. In
this review, we summarize the development of small molecule inhibitors targeting chief proteins in the
DDR pathway, particularly focusing on their implications for cancer therapy. We present the action
mode of DDR molecule inhibitors in preclinical studies and clinical cancer therapy, including monotherapy
and combination therapy with chemotherapeutic drugs or checkpoint suppression therapy.
Keywords: DNA damage response (DDR), DNA repair, small molecule inhibitor, cancer therapy, monotherapy,
combination therapy, synthetic lethal (SL), drug repurposing.
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