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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Small Molecule Inhibitors Targeting Key Proteins in the DNA Damage Response for Cancer Therapy

Author(s): Lulu Li, Alagamuthu Karthick Kumar, Zhigang Hu* and Zhigang Guo*

Volume 28 , Issue 5 , 2021

Published on: 24 February, 2020

Page: [963 - 985] Pages: 23

DOI: 10.2174/0929867327666200224102309

Price: $65

Abstract

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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