South Korean researchers have developed a chemical compound that can diagnose and treat cancer at the same time.
The Korea Research Institute of Bioscience and Biotechnology said on the 17th that a team led by Sung Nak-kyun at its Chemical Biology Research Center has developed BF-04, a new anti-cancer compound that overcomes the limits of existing cancer drugs and allows treatment and real-time diagnosis simultaneously. Existing cancer treatments lose effectiveness because of drug resistance, and it is difficult to confirm how a drug is distributed in the body or how much of it reaches tumor tissue. The team set out to develop a compound to overcome those limits.
The compound works by interfering with the formation of microtubules, which are essential to cell division. Microtubules are thin tube-shaped structures inside cells that move chromosomes when a cell divides. They serve as the ropes or rails that pull chromosomes to either side as a cell splits in two. Rapidly proliferating cancer cells depend heavily on this structure, so when microtubules are disrupted, division can no longer proceed.
The team confirmed that the compound binds to tubulin, the protein that makes up microtubules, and blocks microtubule formation, which in turn suppresses cancer cell division and induces cell death. The compound also proved effective against cancer cells that are resistant to existing microtubule-targeting anti-cancer drugs. The institute said this demonstrates its potential as a new anti-cancer candidate that could complement the limits of existing drugs.
The team also succeeded in imaging the location of tumor tissue and the distribution of the drug by attaching either Cy5, a fluorescent dye, or zirconium-89 (Zr-89), a radioactive isotope used in precision imaging diagnostics. Experiments using cancer organoids cultured from patient tumor tissue, cancer cells and animal models all confirmed the compound's anti-cancer effect and its tumor-targeting properties.
In the animal experiments in particular, the compound accumulated selectively in tumor tissue even without a separate delivery vehicle such as an antibody or nanoparticle. Using molecular imaging equipment, researchers were also able to track in real time how the drug remained in tumor tissue and worked there for up to four days after injection.
The institute said the study is significant because it shows that a therapeutic function that precisely targets cancer cells and a diagnostic function that shows the drug's location in real time can both be developed through a single small chemical compound. It added that this is expected to accelerate an era of patient-tailored precision medicine, in which doctors can immediately confirm whether a drug is being delivered properly, in line with cancer characteristics that differ from patient to patient, and precisely predict treatment response.
Sung, who led the research, said the study is significant in that it has built a new type of integrated cancer diagnosis and treatment platform that combines a powerful therapeutic effect against drug-resistant cancer cells with the ability to observe in real time how a drug is working inside the body. He added that it could be used in various ways in the future development of precision cancer therapies.
The findings were published in the September online edition of Acta Pharmaceutica Sinica B, an international journal in the field of medicinal chemistry.