Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
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- Vittoria Zoppi
- Division of Biological Chemistry and Drug Discovery, School of Life Sciences, James Black Centre, University of Dundee, Dow Street, DD1 5EH, Dundee, Scotland, United Kingdom
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- Scott J. Hughes
- Division of Biological Chemistry and Drug Discovery, School of Life Sciences, James Black Centre, University of Dundee, Dow Street, DD1 5EH, Dundee, Scotland, United Kingdom
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- Chiara Maniaci
- Division of Biological Chemistry and Drug Discovery, School of Life Sciences, James Black Centre, University of Dundee, Dow Street, DD1 5EH, Dundee, Scotland, United Kingdom
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- Andrea Testa
- Division of Biological Chemistry and Drug Discovery, School of Life Sciences, James Black Centre, University of Dundee, Dow Street, DD1 5EH, Dundee, Scotland, United Kingdom
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- Teresa Gmaschitz
- Boehringer Ingelheim RCV GmbH & Co. KG, 1221 Vienna, Austria
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- Corinna Wieshofer
- Boehringer Ingelheim RCV GmbH & Co. KG, 1221 Vienna, Austria
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- Manfred Koegl
- Boehringer Ingelheim RCV GmbH & Co. KG, 1221 Vienna, Austria
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- Kristin M. Riching
- Promega Corporation, 2800 Woods Hollow Road, Madison, Wisconsin 53711, United States
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- Danette L. Daniels
- Promega Corporation, 2800 Woods Hollow Road, Madison, Wisconsin 53711, United States
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- Andrea Spallarossa
- Dipartimento di Farmacia, Sezione di Chimica del Farmaco e del Prodotto Cosmetico, Università degli Studi di Genova, Viale Benedetto XV 3, 16132 Genova, Italy
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- Alessio Ciulli
- Division of Biological Chemistry and Drug Discovery, School of Life Sciences, James Black Centre, University of Dundee, Dow Street, DD1 5EH, Dundee, Scotland, United Kingdom
収録刊行物
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- Journal of Medicinal Chemistry
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Journal of Medicinal Chemistry 62 (2), 699-726, 2018-12-12
American Chemical Society (ACS)