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Updated: Apr 15, 2026

Genome-wide Mapping of Drug-DNA Interactions in Cells with COSMIC Crosslinking of Small Molecules to Isolate Chromatin
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Therapeutic Agents Based on DNA Sequence Specific Binding

Luke Pett1, John A Hartley, Konstantinos Kiakos

  • 1Cancer Research UK Drug- DNA Interactions Research Group, UCL Cancer Institute, Paul O'Gorman Building, 72 Huntley Street, London, WC1E 6BT, UK. luke.pett.12@ucl.ac.uk.

Current Topics in Medicinal Chemistry
|April 14, 2015
PubMed

Insights

New small molecules targeting DNA offer a promising strategy for cancer treatment. These agents aim for increased therapeutic activity and reduced toxicity by selectively interacting with critical genomic sequences.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • DNA-interactive agents have been a cornerstone of cancer chemotherapy.
  • While molecular targeted therapies are advancing, DNA remains a crucial target for anti-cancer drugs.
  • Next-generation agents require enhanced therapeutic efficacy and minimized off-target toxicity.

Purpose of the Study:

  • To evaluate non-covalent DNA-binding small molecules as "gene-control" agents.
  • To explore the potential of sequence-selective agents for targeting critical genomic sites.
  • To review natural products and synthetic derivatives with sequence-specific DNA-covalent modification activity.

Main Methods:

  • Evaluation of non-covalent DNA binding small molecules.
  • Exploitation of inherent or engineered DNA sequence selectivity.
  • Review of natural products and synthetic derivatives acting via DNA-covalent modification.

Main Results:

  • Non-covalent DNA binding small molecules show potential as gene-control agents.
  • Sequence selectivity is key for targeting critical genomic sequences.
  • Various natural and synthetic compounds exhibit sequence-specific DNA-covalent modification.

Conclusions:

  • Non-covalent DNA-binding small molecules represent a viable strategy for next-generation cancer therapy.
  • Targeting DNA with sequence-selective agents can improve therapeutic outcomes.
  • Further research into these agents may lead to more effective and safer cancer treatments.

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