Conventional targeted drugs, RNA drugs, and radiopharmaceuticals: targeting from drivers to passengers

Yichi Huang; Ting Huang; Saijun Fan; Yu Zhao

doi:10.55092/exrna20240010

Review

Open Access

Conventional targeted drugs, RNA drugs, and radiopharmaceuticals: targeting from drivers to passengers

Yichi Huang^†Ting Huang^†Saijun FanYu Zhao^∗

Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin 300192, China

†These two authors contributed equally.

* zhaoyu@irm-cams.ac.cn

Volume
Volume 6 Issue 2, 2024
Citation
Huang Y, Huang T, Fan S, Zhao Y. Conventional targeted drugs, RNA drugs, and radiopharmaceuticals: targeting from drivers to passengers. ExRNA 2024(2):0010, https://doi.org/10.55092/exrna20240010.
DOI
10.55092/exrna20240010
Copyright
Copyright2024 by the authors. Published by ELSP.

Abstract

Targeted therapy targets the driver genes of tumor cells and effective inhibitors were developed to treat tumors by inhibiting tumor cell proliferation, interfering with the cell cycle, inducing tumor cell apoptosis, and inhibiting tumor angiogenesis. The emergence of RNA therapeutics provides more opportunities to target some driver genes which cannot be targeted with conventional drugs. However, the response of these targeted drugs in patients may be limited by their potential drug toxicity and tolerance. With the development of positron emission tomography (PET) and molecular biology, a number of passenger genes that do not have a driving role in tumor growth such as prostate-specific membrane antigen (PSMA) in prostate cancer, have been developed for widespread use in the diagnosis and treatment of cancer through radiolabeled molecular tracers. Radiopharmaceutical targets exhibit high specificity, which contributes to enhancing inhibitory activity in tumor but avoiding toxic effects on normal tissues. In addition, these radiopharmaceuticals have been continuously upgraded through chemical structure optimization such as regulating linkage lengths, hydrophobicity and charge, introducing albumin-binding entities and increasing the amphiphilicity of tracers enables radiopharmaceuticals to traverse cell and nuclear membranes, which have further improved diagnostic sensitivity/therapeutic specificity and reduced off-target toxicity.

Keywords

targeted drugs; RNA drugs; radiopharmaceuticals; driver genes; passenger genes

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