targeting aquaporin function potent inhibition of aquaglyceroporin-3 by a gold-based compound针对水通道蛋白功能强大的抑制aquaglyceroporin-3的黄金为基础的化合物.pdf

Targeting Aquaporin Function: Potent Inhibition of Aquaglyceroporin-3 by a Gold-Based Compound 1 2 2 ´ 3 ´ 3 Ana Paula Martins , Alessandro Marrone , Antonella Ciancetta , Ana Galan Cobo , Miriam Echevarrıa , Teresa F. Moura1, Nazzareno Re2, Angela Casini4*, Grac¸a Soveral1,5* ´ ˆ 1 REQUIMTE, Departamento de Quımica, Faculdade de Ciencias e Tecnologia, Universidade Nova de Lisboa, Caparica, Portugal, 2 Dipartimento di Scienze del Farmaco, ` ´ Universita G. d’Annunzio, Chieti, Italy, 3 Instituto de Biomedicina de Sevilla (IBiS), Hospital Universitario Virgen del Rocıo/CSIC/Universidad de Sevilla, Seville, Spain, ´ 4 Pharmacokinetics, Toxicology and Targeting, Research Institute of Pharmacy, University of Groningen, Groningen, The Netherlands, 5 Departamento de Bioquımica e ´ Biologia Humana, Faculdade de Farmacia, Universidade de Lisboa, Lisbon, Portugal 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 screene