ArticlePloS one2012
Targeting aquaporin function: potent inhibition of aquaglyceroporin-3 by a gold-based compound.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 60 papers.
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Who cites it
60 citing papers in PubMed, 152 citations in OpenAlex.
- Aquaporin-3 and aquaporin-5 impact the development of pancreatic ductal adenocarcinoma spheroids.FEBS open bio · 2026Article
- Aquaporin membrane channels in the hepatobiliary tract: a model of complexity and clinical implications in health and disease.Internal and emergency medicine · 2026Review
- Aquaporin-1, aquaporin-3 and aquaporin-5 differentially modulate cell biophysical and biomechanical properties, impacting cell stiffness and cell-cell adhesion.The FEBS journal · 2026Article
- Aquaporins: a novel perspective in the treatment of lung diseases.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2025Review
- Narrowed pore conformations of aquaglyceroporins AQP3 and GlpF.Nature communications · 2025Article
- The Expanding Role of Aquaporin-1, Aquaporin-3 and Aquaporin-5 as Transceptors: Involvement in Cancer Development and Potential Druggability.International journal of molecular sciences · 2025Review
- Exploring Aquaporins in Human Studies: Mechanisms and Therapeutic Potential in Critical Illness.Life (Basel, Switzerland) · 2024Review
- Liposomal Formulation of an Organogold Complex Enhancing Its Activity as Antimelanoma Agent-In Vitro and In Vivo Studies.Pharmaceutics · 2024Article
- To quest new targets ofJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2024Review
- Eliminating malaria transmission requires targeting immature and mature gametocytes through lipoidal uptake of antimalarials.Nature communications · 2024Article
- Characterization of human aquaporin ion channels in a yeast expression system as a tool for novel ion channel discovery.Bioscience reports · 2024Article
- Evaluation of the Mammalian Aquaporin Inhibitors Auphen and Z433927330 in Treating Breast Cancer.Cancers · 2024Article
- Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators.Marine drugs · 2024Article
- Aquaporin Modulation by Cations, a Review.Current issues in molecular biology · 2024Review
- Discrimination between the effects of pulsed electrical stimulation and electrochemically conditioned medium on human osteoblasts.Journal of biological engineering · 2023Article
- Unraveling the Aquaporin-3 Inhibitory Effect of Rottlerin by Experimental and Computational Approaches.International journal of molecular sciences · 2023Article
- Aquaporin-mediated dysregulation of cell migration in disease states.Cellular and molecular life sciences : CMLS · 2023Review
- Methods for studying mammalian aquaporin biology.Biology methods & protocols · 2023Review
- Aquaporin Inhibitors.Advances in experimental medicine and biology · 2023Article
- Review
Corrections and comments
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Authors and funding
9 authors at 6 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Aquaporins (AQPs) are membrane channels that conduct water and small solutes such as glycerol and are involved in many physiological functions. Aquaporin-based modulator drugs are predicted to be of broad potential utility in the treatment of several diseases. Until today few AQP inhibitors have been described as suitable candidates for clinical development. Here we report on the potent inhibition of AQP3 channels by gold(III) complexes screened on human red blood cells (hRBC) and AQP3-transfected PC12 cells by a stopped-flow method. Among the various metal compounds tested, Auphen is the most active on AQP3 (IC(50) = 0.8±0.08 µM in hRBC). Interestingly, the compound poorly affects the water permeability of AQP1. The mechanism of gold inhibition is related to the ability of Au(III) to interact with sulphydryls groups of proteins such as the thiolates of cysteine residues. Additional DFT and modeling studies on possible gold compound/AQP adducts provide a tentative description of the system at a molecular level. The mapping of the periplasmic surface of an homology model of human AQP3 evidenced the thiol group of Cys40 as a likely candidate for binding to gold(III) complexes. Moreover, the investigation of non-covalent binding of Au complexes by docking approaches revealed their preferential binding to AQP3 with respect to AQP1. The high selectivity and low concentration dependent inhibitory effect of Auphen (in the nanomolar range) together with its high water solubility makes the compound a suitable drug lead for future in vivo studies. These results may present novel metal-based scaffolds for AQP drug development.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.