New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the hydroxytriazole scaffold

Autor: Pippione, A.C., Kilic-Kurt, Z., Kovachka, S., Sainas, S., Rolando, B., Denasio, E., Pors, Klaus, Adinolfi, S., Zonari, D., Bagnati, R., Lolli, M.L., Spyrakis, F., Oliaro-Bosso, S., Boschi, D.

Yes
The aldo-keto reductase 1C3 (AKR1C3) enzyme is considered an attractive target in Castration Resistant Prostate Cancer (CRPC) because of its role in the biosynthesis of androgens. Flufenamic acid, a non-selective AKR1C3 inhibitor, has previo

Externí odkaz: http://hdl.handle.net/10454/19070

Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer.

Autor: Pippione AC; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Kovachka S; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy; The Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, Jupiter, FL, USA., Vigato C; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Bertarini L; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy; Department of Life Sciences, University of Modena and Reggio Emilia, via Campi 103, 41125, Modena, Italy., Mannella I; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Sainas S; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Rolando B; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Denasio E; Institute of Cancer Therapeutics, Faculty of Life Sciences, University of Bradford, West Yorkshire, BD7 1DP, UK., Piercy-Mycock H; Institute of Cancer Therapeutics, Faculty of Life Sciences, University of Bradford, West Yorkshire, BD7 1DP, UK., Romalho L; Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, DK-2100, Copenhagen, Denmark., Salladini E; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Adinolfi S; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Zonari D; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Peraldo-Neia C; Laboratory of Cancer Genomics, Fondazione Edo ed Elvo Tempia, via Malta 3, 13900, Biella, Italy., Chiorino G; Laboratory of Cancer Genomics, Fondazione Edo ed Elvo Tempia, via Malta 3, 13900, Biella, Italy., Passoni A; Department of Environmental Health Sciences, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156, Milan, Italy., Mirza OA; Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, DK-2100, Copenhagen, Denmark., Frydenvang K; Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, DK-2100, Copenhagen, Denmark., Pors K; Institute of Cancer Therapeutics, Faculty of Life Sciences, University of Bradford, West Yorkshire, BD7 1DP, UK., Lolli ML; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Spyrakis F; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy., Oliaro-Bosso S; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy. Electronic address: simona.oliaro@unito.it., Boschi D; Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, 10125, Turin, Italy. Electronic address: donatella.boschi@unito.it.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2024 Mar 15; Vol. 268, pp. 116193. Date of Electronic Publication: 2024 Feb 07.

Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach

Autor: Pippione, A.C., Giraudo, A., Bonanni, D., Carnovale, I.M., Marini, E., Cena, C., Costale, A., Zonari, D., Pors, Klaus, Sadiq, Maria, Boschi, D., Oliaro-Bosso, S., Lolli, M.L.

Yes
The aldo-keto reductase 1C3 isoform (AKR1C3) plays a vital role in the biosynthesis of androgens, making this enzyme an attractive target for castration-resistant prostate cancer therapy. Although AKR1C3 is a promising drug target, no AKR1C3

Externí odkaz: http://hdl.handle.net/10454/13966

Effects of the Molecular Weight of Hyaluronic Acid in a Carbon Nanotube Drug Delivery Conjugate.

Autor: Arpicco S; Department of Drug Science and Technology, University of Torino, Turin, Italy., Bartkowski M; School of Chemical Sciences, Dublin City University (DCU), Dublin, Ireland., Barge A; Department of Drug Science and Technology, University of Torino, Turin, Italy., Zonari D; Department of Drug Science and Technology, University of Torino, Turin, Italy., Serpe L; Department of Drug Science and Technology, University of Torino, Turin, Italy., Milla P; Department of Drug Science and Technology, University of Torino, Turin, Italy., Dosio F; Department of Drug Science and Technology, University of Torino, Turin, Italy., Stella B; Department of Drug Science and Technology, University of Torino, Turin, Italy., Giordani S; School of Chemical Sciences, Dublin City University (DCU), Dublin, Ireland.

Publikováno v: Frontiers in chemistry [Front Chem] 2020 Dec 14; Vol. 8, pp. 578008. Date of Electronic Publication: 2020 Dec 14 (Print Publication: 2020).

Pentamidine-Loaded Lipid and Polymer Nanocarriers as Tunable Anticancer Drug Delivery Systems.

Autor: Stella B; Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via P. Giuria 9, 10125, Torino, Italy. Electronic address: barbara.stella@unito.it., Andreana I; Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via P. Giuria 9, 10125, Torino, Italy., Zonari D; Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via P. Giuria 9, 10125, Torino, Italy., Arpicco S; Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via P. Giuria 9, 10125, Torino, Italy. Electronic address: silvia.arpicco@unito.it.

Publikováno v: Journal of pharmaceutical sciences [J Pharm Sci] 2020 Mar; Vol. 109 (3), pp. 1297-1302. Date of Electronic Publication: 2019 Nov 18.