Drug intelligence / Profile preview

d-lys6-lhrh-curcumin

Development stage
Preclinical
Lead developer
University of South Dakota
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intravenous
01

Overview

d-lys6-lhrh-curcumin is a synthetic peptide-drug conjugate consisting of a luteinizing hormone-releasing hormone (LHRH) analog ([DLys^6^-LHRH]) covalently linked via glutaric acid esterification to curcumin, a polyphenolic compound derived from turmeric. The conjugate is designed for targeted therapy of cancers expressing LHRH receptors, specifically pancreatic ductal adenocarcinoma. The mechanism involves the LHRH analog serving as a targeting moiety to deliver curcumin directly to LHRH receptor-expressing tumor cells, increasing local anticancer effects and improving water solubility compared to free curcumin, thus enabling intravenous administration. This conjugate inhibits proliferation and induces apoptosis of pancreatic cancer cells via caspase-3 activation and PARP cleavage, with efficacy demonstrated both in vitro and in vivo. Curcumin released at the tumor site inhibits survival pathways (such as NF-κB). This molecule is not yet approved for clinical use and is primarily characterized in preclinical research.[1][2]

Other names
DLys^6^-LHRH-CurcuminDLys(6)-LHRH-curcumin
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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