GnRH-III[8Lys(Dau=Aoa)]

**GnRH-III[8Lys(Dau=Aoa)]** is a peptide-drug conjugate consisting of the lamprey-derived gonadotropin-releasing hormone III (GnRH-III) peptide, modified at the 8th lysine residue with an aminooxyacetyl group, to which the cytotoxic drug daunorubicin is covalently bound via an oxime bond[1][2][3][4]. The conjugate targets tumors expressing the GnRH receptor (GnRH-R), which are highly expressed in several cancer types, including breast and colon cancer. Upon receptor-mediated endocytosis, the drug is delivered into tumor cells, where lysosomal degradation releases an active metabolite capable of binding DNA and exerting a cytotoxic effect[1][2]. The modification at Lys8 enables stable drug linkage, retains binding affinity for tumor-expressed GnRH-R, and enhances cellular uptake. The drug is designed for *targeted chemotherapy* to increase selectivity and reduce daunorubicin-related systemic toxicity, and demonstrates significant in vitro and in vivo antitumor activity[1][2][3]. Most research and development have focused on preclinical applications in cancer, particularly colon and breast cancer.

Other names

Dau-GnRH-IIIGnRH-III–[8Lys(Dau=Aoa)]GnRH-III(8Lys(Dau=Aoa))oxime bond-linked daunorubicin-GnRH-III