Drug intelligence / Profile preview

[Ac-D2Nal1, D-4Cpa2, D-3Pal3, D-Lys6, D-Ala10]GnRH-II

Development stage
Preclinical
Modality
Peptides, Small Molecules
Administration
Parenteral
01

Overview

**[Ac-D2Nal1, D-4Cpa2, D-3Pal3, D-Lys6, D-Ala10]GnRH-II** is a synthetic decapeptide antagonist of the Gonadotropin-Releasing Hormone II (GnRH-II) receptor, featuring specific substitutions at positions 1 (D-2-naphthylalanyl), 2 (D-4-chlorophenylalanine), 3 (D-3-pyridylalanine), 6 (D-lysine), and 10 (D-alanine)[1][2]. It was designed to **increase peptide stability and receptor selectivity** by incorporating D-amino acids, thereby resisting degradation and avoiding receptor activation.[2] This compound **induces apoptosis and inhibits the growth of tumor cells** in preclinical models of human endometrial, ovarian, and breast cancer by antagonizing GnRH-II signaling[1][2]. Its **mechanism of action involves binding to the GnRH-II receptor**, blocking endogenous GnRH-II and consequently interfering with downstream signaling involved in tumor proliferation and survival[1]. It is not a marketed pharmaceutical and remains an experimental tool in oncology research with published antitumoral effects demonstrated in cell culture and animal models[1][2]. The developer and manufacturer information is not provided in the literature and the drug appears to have been synthesized and characterized in academic settings[1][2].

Other names
GnRH-ant-II analogSynthetic GnRH-II antagonist (D-naphthylalanyl, D-4-chlorophenylalanine, D-3-pyridylalanine, D-lysine, D-alanine substituted)
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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