Systematic Investigation of the Permeability of Androgen Receptor PROTACs.
Scott, Duncan E
Rooney, Timothy PC
Bayle, Elliott D
Willems, Henriette MG
Clarke, Jonathan H
Andrews, Stephen P
ACS Med Chem Lett
American Chemical Society (ACS)
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Scott, D. E., Rooney, T. P., Bayle, E. D., Mirza, T., Willems, H. M., Clarke, J. H., Andrews, S. P., & et al. (2020). Systematic Investigation of the Permeability of Androgen Receptor PROTACs.. ACS Med Chem Lett, 11 (8), 1539-1547. https://doi.org/10.1021/acsmedchemlett.0c00194
Bifunctional molecules known as PROTACs simultaneously bind an E3 ligase and a protein of interest to direct ubiquitination and clearance of that protein, and they have emerged in the past decade as an exciting new paradigm in drug discovery. In order to investigate the permeability and properties of these large molecules, we synthesized two panels of PROTAC molecules, constructed from a range of protein-target ligands, linkers, and E3 ligase ligands. The androgen receptor, which is a well-studied protein in the PROTAC field was used as a model system. The physicochemical properties and permeability of PROTACs are discussed.
This work was funded by Alzheimer’s Research UK (grant: ARUK-2015DDI-CAM), with support from the ALBORADA Trust. The ALBORADA Drug Discovery Institute is core funded by Alzheimer’s Research UK (registered charity No. 1077089 and SC042474).
Alzheimer's Research UK (ARUK-2015DDI-CAM)
External DOI: https://doi.org/10.1021/acsmedchemlett.0c00194
This record's URL: https://www.repository.cam.ac.uk/handle/1810/306747
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