Linker Optimization and Therapeutic Evaluation of Phosphatidylserine-Targeting Zinc Dipicolylamine-based Drug Conjugates

Yu-Wei Liu, Yunyu Chen, Chia‐Yu Hsu, Tai‐Yu Chiu, Kuan-Liang Liu, Chen‐Fu Lo, Mingyu Fang, Yucheng Huang, Teng‐Kuang Yeh, Koon Y. Pak,

Journal of Medicinal Chemistry · 2019 · 15 citations · 34 references

Concepts

Abstract

not only induced regressions in colorectal and pancreatic tumor models, it also exhibited at least 5-fold enhancement in antitumor efficacy with only 40% of the drug employed during treatment, culminating in a >12.5-fold increase in therapeutic potential. Our study discloses a chemically distinct apoptosis-targeting theranostic, with built-in complementary functional moieties between the targeting module and the drug mechanism to expand the arsenal of antitumor therapy.

References

34