Photodynamic Oncotherapy Mediated by Gonadotropin-Releasing Hormone Receptors

Peng Xu; Yuhua Jia; Yongshuai Yang; Jincan Chen; Ping Hu; Zhuo Chen; Mingdong Huang

doi:10.1021/acs.jmedchem.7b01216

Photodynamic Oncotherapy Mediated by Gonadotropin-Releasing Hormone Receptors

J Med Chem. 2017 Oct 26;60(20):8667-8672. doi: 10.1021/acs.jmedchem.7b01216. Epub 2017 Oct 10.

Authors

Peng Xu¹, Yuhua Jia^{1

2}, Yongshuai Yang^{1

2}, Jincan Chen¹, Ping Hu¹, Zhuo Chen¹, Mingdong Huang^{1

3}

Affiliations

¹ State Key Laboratory of Structural Chemistry and Danish-Chinese Centre for Proteases and Cancer, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences , Fuzhou, Fujian 350002, P. R. China.
² College of Life Science, Fujian Agriculture and Forestry University , Fuzhou, Fujian 350002, P. R. China.
³ College of Chemistry, Fuzhou University , Fuzhou, Fujian 350116, P. R. China.

PMID: 28968084
DOI: 10.1021/acs.jmedchem.7b01216

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Breast Neoplasms / drug therapy*
Breast Neoplasms / pathology
Cell Line, Tumor
Female
Fluorescence
Gonadotropin-Releasing Hormone / physiology*
Humans
Mice
Microscopy, Confocal
Photochemotherapy*
Xenograft Model Antitumor Assays

Substances

Gonadotropin-Releasing Hormone