Cancer Radiosensitizers

Trends Pharmacol Sci. 2018 Jan;39(1):24-48. doi: 10.1016/j.tips.2017.11.003. Epub 2017 Dec 7.

Abstract

Radiotherapy (RT) is a mainstay treatment for many types of cancer, although it is still a large challenge to enhance radiation damage to tumor tissue and reduce side effects to healthy tissue. Radiosensitizers are promising agents that enhance injury to tumor tissue by accelerating DNA damage and producing free radicals. Several strategies have been exploited to develop highly effective and low-toxicity radiosensitizers. In this review, we highlight recent progress on radiosensitizers, including small molecules, macromolecules, and nanomaterials. First, small molecules are reviewed based on free radicals, pseudosubstrates, and other mechanisms. Second, nanomaterials, such as nanometallic materials, especially gold-based materials that have flexible surface engineering and favorable kinetic properties, have emerged as promising radiosensitizers. Finally, emerging macromolecules have shown significant advantages in RT because these molecules can be combined with biological therapy as well as drug delivery. Further research on the mechanisms of radioresistance and multidisciplinary approaches will accelerate the development of radiosensitizers.

Keywords: cancer radiosensitizer; macromolecules; nanomaterials; small molecules.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Humans
  • Metal Nanoparticles / chemistry
  • Metal Nanoparticles / therapeutic use
  • Neoplasms / radiotherapy*
  • Radiation-Sensitizing Agents / chemistry*
  • Radiation-Sensitizing Agents / pharmacology
  • Radiation-Sensitizing Agents / therapeutic use
  • Radiotherapy / methods

Substances

  • Antineoplastic Agents
  • Radiation-Sensitizing Agents