Drug intelligence / Profile preview

Auphen

Development stage
Preclinical
Lead developer
Università degli Studi Gabriele d'Annunzio Chieti e Pescara
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Auphen is a gold(III) coordination complex, chemically represented as [Au(1,10-phenanthroline)Cl2]Cl. It is a potent and selective inhibitor of aquaglyceroporins, particularly aquaporin-3 (AQP3) and aquaporin-7 (AQP7). By binding to sulfhydryl groups of cysteine residues (such as Cys40 in AQP3), Auphen blocks the transport of water, glycerol, and hydrogen peroxide (H2O2) across cell membranes. It is widely utilized as a chemical probe in research to investigate the physiological roles of aquaporins. Preclinical studies have explored its potential therapeutic applications in various cancers (including breast cancer, melanoma, and hepatocellular carcinoma) where AQP3 is overexpressed, as well as in malaria, where it targets host aquaporin-3 to inhibit Plasmodium parasite development.

Other names
[Au(1,10-phenanthroline)Cl2]Cl[Au(phen)Cl2]Cl[AuCl2(phen)]+Cl-Auphen chloridedichloro(1,10-phenanthroline)gold(III) chloridegold(III) (1,10-phenanthroline) chloride
02

Targets

AQP9 (Aquaporin-9)AQP3 (Aquaporin-3 channel protein)PfAQP (Plasmodium falciparum aquaglyceroporin)AQP7 (Aquaporin-7)

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