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

Lulu Li1, Alagamuthu Karthick Kumar1, Zhigang Hu1

  • 1Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Sciences, Nanjing Normal University, 1 WenYuan Road, Nanjing 210023, China.

Current Medicinal Chemistry
|February 25, 2020
PubMed

Insights

Targeting DNA damage response (DDR) proteins with small molecule inhibitors offers a promising cancer therapy strategy. This review details DDR inhibitors

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • The DNA damage response (DDR) pathway is crucial for maintaining genomic stability.
  • Defects in DDR pathways can lead to cancer susceptibility and resistance.
  • Aberrant protein expression within DDR, particularly DNA repair, is linked to cancer cell survival.

Purpose of the Study:

  • To review the development of small molecule inhibitors targeting key DDR proteins.
  • To explore the therapeutic implications of these inhibitors in cancer treatment.
  • To summarize their mechanisms of action in preclinical and clinical settings.

Main Methods:

  • Literature review of small molecule inhibitors targeting DDR proteins.
  • Analysis of preclinical studies on DDR inhibitor efficacy.
  • Examination of clinical trial data for DDR inhibitors in monotherapy and combination treatments.

Main Results:

  • Small molecule inhibitors targeting DDR proteins show significant therapeutic potential.
  • These inhibitors can be used as monotherapy or in combination with chemotherapy or checkpoint inhibitors.
  • Understanding the action mode of DDR inhibitors is key to optimizing cancer therapy.

Conclusions:

  • Targeting DDR proteins with small molecule inhibitors is an effective cancer therapeutic strategy.
  • Further research into DDR inhibitors can lead to novel cancer treatments.
  • Combination therapies involving DDR inhibitors demonstrate promise for overcoming cancer resistance.

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