Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 20, Pages 8667-8672Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01216
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Funding
- National Natural Science Foundation of China [21708043, 81572944, U1405229]
- CAS/SAFEA International Partnership Program for Creative Research Teams
- Scientific Equipment Development Project of the CAS [XDA09030307]
- CAS Cross-Disciplinary & Collaborative Research Team Program
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Here, we report photodynamic oncotherapies mediated by gonadotropin-releasing hormone (GnRH) receptors. We synthesized conjugates 1 and 2 by coupling zinc phthalocyanine (ZnPc) to GnRH analogues. Compared to unmodified ZnPc, conjugates 1 and 2 exhibited higher and more specific phototoxicities to breast cancer cells. Furthermore, the two conjugates demonstrated excellent antitumor efficacies in a breast cancer-grafted animal model. Biodistribution study suggested the high biosafety of conjugate 2 because of the low retention in brain and skin.
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