Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC

Abstract Targeting the estrogen receptor alpha (ERα) pathway is validated in the clinic as an effective means to treat ER+ breast cancers. Here we present the development of a VHL-targeting and orally bioavailable proteolysis-targeting chimera (PROTAC) degrader of ERα. In vitro studies with this PRO...

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Bibliografiske detaljer

Principais autores:	Thomas G. Hayhow, Beth Williamson, Mandy Lawson, Natalie Cureton, Erin L. Braybrooke, Andrew Campbell, Rodrigo J. Carbajo, Azadeh Cheraghchi-Bashi, Elisabetta Chiarparin, Coura R. Diène, Charlene Fallan, David I. Fisher, Frederick W. Goldberg, Lorna Hopcroft, Philip Hopcroft, Anne Jackson, Jason G. Kettle, Teresa Klinowska, Ulrike Künzel, Gillian Lamont, Hilary J. Lewis, Gareth Maglennon, Scott Martin, Pablo Morentin Gutierrez, Christopher J. Morrow, Myria Nikolaou, J. Willem M. Nissink, Patrick O’Shea, Radoslaw Polanski, Markus Schade, James S. Scott, Aaron Smith, Judith Weber, Joanne Wilson, Bin Yang, Claire Crafter
Format:	Artigo
Sprog:	Inglês
Udgivet:	Nature Portfolio 2024-05-01
Serier:	Communications Biology
Online adgang:	https://doi.org/10.1038/s42003-024-06238-x
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