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Updated: Jun 16, 2026
Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
Screening DNA-targeted anticancer drug in vitro based on the drug-conjugated DNA by resonance light scattering
Zhanguang Chen1, Tianhe Song, Shaobin Wang
1Department of Chemistry, Shantou University, Daxue Road 243#, Shantou 515063, China. kqlu@stu.edu.cn
Abstract:
A sensitive and reliable assay has been developed to directly screen DNA-targeted anticancer drugs in vitro via using resonance light scattering (RLS) technique. The results of experiments displayed that the increment of RLS intensity was directly proportional to the antitumor effect of anticancer drugs. Through the RLS spectra, the activities of four drugs have been demonstrated as mitoxantrone (MIT)>epirarubicin (EPI)>daunorubicin (DAU)>adriamycin (ADM). However, to further verify the activities of the above four drugs, binding constant (k) for each of them has been calculated by RLS technique as follows: k(RLS) (MIT, 8.75 x 10(5) L mol(-1))>k(RLS) (EPI, 6.58 x 10(5) L mol(-1))>k(RLS) (DAU, 4.79 x 10(5) L mol(-1))>k(RLS) (ADM, 3.82 x 10(5) L mol(-1)). Also, this RLS assay result was validated by seasoned vitro screening methods for anticancer drugs. In all, the proposed RLS is not only a simple, sensitive, objective and straightforward method, but also it is an unprecedented assay for primarily screening DNA-targeted anticancer drugs.
Insights
A new resonance light scattering (RLS) assay offers a simple and sensitive method for screening DNA-targeted anticancer drugs. This technique accurately quantifies drug activity and binding constants, aiding in the development of novel cancer therapies.
Area of Science:
- Analytical Chemistry
- Biochemistry
- Pharmacology
Background:
- Developing sensitive and reliable assays for screening DNA-targeted anticancer drugs is crucial for cancer therapy.
- Existing methods for evaluating drug efficacy can be complex and time-consuming.
Purpose of the Study:
- To develop and validate a novel resonance light scattering (RLS) assay for the direct screening of DNA-targeted anticancer drugs.
- To establish the correlation between RLS intensity and the antitumor effect of various drugs.
Main Methods:
- Utilized the resonance light scattering (RLS) technique to develop a new assay for DNA-targeted anticancer drugs.
- Measured RLS intensity changes in response to drug interactions with DNA.
- Calculated binding constants (k) for selected anticancer drugs using the RLS assay.
Main Results:
- RLS intensity directly correlated with the antitumor efficacy of the tested drugs.
- Drug activity was ranked as mitoxantrone (MIT) > epirubicin (EPI) > daunorubicin (DAU) > adriamycin (ADM) based on RLS spectra.
- Calculated binding constants validated the drug activity ranking: k(MIT) > k(EPI) > k(DAU) > k(ADM).
- The RLS assay results were consistent with established in vitro screening methods.
Conclusions:
- The proposed RLS assay is a simple, sensitive, objective, and straightforward method for screening DNA-targeted anticancer drugs.
- This RLS assay represents an unprecedented approach for the primary screening of potential anticancer agents.
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