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Review
. 2021 Feb 12:16:1083-1102.
doi: 10.2147/IJN.S290438. eCollection 2021.

Application of Radiosensitizers in Cancer Radiotherapy

Liuyun Gong  1 , Yujie Zhang  2   3 , Chengcheng Liu  2 , Mingzhen Zhang  2   3 , Suxia Han  1
Affiliations
Review

Application of Radiosensitizers in Cancer Radiotherapy

Liuyun Gong et al. Int J Nanomedicine. .

Erratum in

Abstract

Radiotherapy (RT) is a cancer treatment that uses high doses of radiation to kill cancer cells and shrink tumors. Although great success has been achieved on radiotherapy, there is still an intractable challenge to enhance radiation damage to tumor tissue and reduce side effects to healthy tissue. Radiosensitizers are chemicals or pharmaceutical agents that can enhance the killing effect on tumor cells by accelerating DNA damage and producing free radicals indirectly. In most cases, radiosensitizers have less effect on normal tissues. In recent years, several strategies have been exploited to develop radiosensitizers that are highly effective and have low toxicity. In this review, we first summarized the applications of radiosensitizers including small molecules, macromolecules, and nanomaterials, especially those that have been used in clinical trials. Second, the development states of radiosensitizers and the possible mechanisms to improve radiosensitizers sensibility are reviewed. Third, the challenges and prospects for clinical translation of radiosensitizers in oncotherapy are presented.

Keywords: cancer radiotherapy; mechanism; nanomedicine; radiosensitizers; therapeutics.

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Conflict of interest statement

The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
Schematic of the mechanism of ionizing radiation (IR) in RT. In the case of direct effect, IR directly damages the DNA, which, if unrepaired, results in cell death or permanent growth arrest. In the case of indirect effect, ROS are formed by the radiolysis of a large amount of water and oxygen, and then the ROS damage the DNA. There are many types of DNA damage, such as base change, SSB, DSB, cross-linkage with protein or with other DNA molecules.
Figure 2
Figure 2
Molecular structures of some representative small-molecule radiosensitizers discussed in this paper.
Figure 3
Figure 3
Radiosensitization mechanism of macromolecules. (A) Proteins and peptides. (a1) Direct interaction of key proteins. (a2) Loading of radioactive seeds. (a3) Radiosensitizers delivery. (a4) Conjugation with nanomaterials. (B) miRNAs can then bind with mRNAs to implement radiosensitization. (b1) Downregulation by inhibitors. (b2) Upregulation. (C) siRNAs can improve radiosensitivity by binding and degrading complementary mRNAs. (D) Oligonucleotides improve the radiosensitivity by complementary binding with DNAs.
Figure 4
Figure 4
Radiosensitization mechanism of metal-based nanomaterials. The process contains physical and biochemical sensitization mechanism.
See this image and copyright information in PMC

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