4 years ago

Photodynamic Oncotherapy Mediated by Gonadotropin-Releasing Hormone Receptors

Photodynamic Oncotherapy Mediated by Gonadotropin-Releasing Hormone Receptors
Jincan Chen, Yongshuai Yang, Peng Xu, Mingdong Huang, Ping Hu, Zhuo Chen, Yuhua Jia
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.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b01216

DOI: 10.1021/acs.jmedchem.7b01216

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