Recent Developments Using Small Molecules to Target RAD51: How to Best Modulate RAD51 for Anticancer Therapy?

Brian Budke, Wei Lv, Alan P. Kozikowski, Philip P. Connell

Research output: Contribution to journalComment/debatepeer-review

Abstract

Homologous recombination (HR) is an evolutionarily conserved DNA repair process. Overexpression of the key HR protein RAD51 is a common feature of malignant cells. RAD51 plays two distinct genome-stabilizing roles, including HR-mediated repair of double-strand breaks (DSBs) and the promotion of replication fork stability during replication stress. Because upregulation of RAD51 in cancer cells can promote tumor resistance to DNA-damaging oncologic therapies, we and others have worked to develop cancer therapeutics that target various aspects of RAD51 protein function. Herein, we provide an overview of recent developments in this field, together with our perspectives on the challenges associated with these evolving anticancer strategies.

Original languageEnglish (US)
Pages (from-to)2468-2473
Number of pages6
JournalChemMedChem
Volume11
Issue number22
DOIs
StatePublished - Nov 21 2016

Keywords

  • RAD51
  • cancer therapy
  • drug discovery
  • homologous recombination
  • medicinal chemistry

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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