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GnRH-III[4Lys(Bu),8Lys(Dau=Aoa)]
- Development stage
- Preclinical
- Lead developer
- Eötvös Loránd University
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous, Intraperitoneal
01
Overview
**GnRH-III[4Lys(Bu),8Lys(Dau=Aoa)]**, also called **K2**, is a preclinical gonadotropin-releasing hormone III peptide-drug conjugate developed by Hungarian academic researchers for receptor-targeted cancer therapy. It uses a GnRH-III peptide ligand to bind gonadotropin-releasing hormone receptors on tumor cells; daunorubicin is covalently attached to Lys8 through an aminooxyacetyl-derived oxime linkage, while butyrate is attached to Lys4. Receptor-mediated uptake and lysosomal degradation release a daunorubicin-containing cytotoxic metabolite that damages DNA and promotes cancer-cell death. The conjugate showed antitumor activity in colorectal carcinoma and breast-carcinoma models, including tumor-growth inhibition and reduced neovascularization in an orthotopic colorectal-cancer mouse model. ([mdpi.com](https://www.mdpi.com/1999-4923/10/4/223))
- Other names
- GnRH-III-[4Lys(Bu),8Lys(Dau=Aoa)]GnRH-III[4Lys(Bu),8Lys(Dau=Aoa)]K2K-2K 2
02
Targets
TOP2A (DNA topoisomerase II)HDAC (HDAC family)GnRHR (Gonadotropin-releasing hormone receptor)DNA
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