PROTAC Cell Permeability and Oral Bioavailability: A Journey Into Uncharted Territory

Future Medicinal ChemistryVol. 14, No. 3 EditorialPROTAC cell permeability and oral bioavailability: a journey into uncharted territoryVasanthanathan Poongavanam & Jan KihlbergVasanthanathan Poongavanam https://orcid.org/0000-0002-8880-9247Department of Chemistry - BMC, Uppsala University, SE-75123, Uppsala, SwedenSearch for more papers by this author & Jan Kihlberg *Author for correspondence: E-mail Address: jan.kihlberg@kemi.uu.sehttps://orcid.org/0000-0002-4205-6040Department of Chemistry - BMC, Uppsala University, SE-75123, Uppsala, SwedenSearch for more papers by this authorPublished Online:29 Sep 2021https://doi.org/10.4155/fmc-2021-0208AboutSectionsView ArticleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinkedInReddit View articleKeywords: ADME/Toxdrug designin vitro assaysmolecular chameleonoral druggable spaceReferences1. Edmondson SD, Yang B, Fallan C. 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Chem. 64, 8042–8052 (2021).Crossref, Medline, CAS, Google ScholarFiguresReferencesRelatedDetailsCited ByDesign, synthesis and bioactivity evaluation of self-assembled PROTACs based on multi-target kinase inhibitorsBioorganic Chemistry, Vol. 134Trends in Molecular Properties, Bioavailability, and Permeability across the Bayer Compound Collection8 February 2023 | Journal of Medicinal Chemistry, Vol. 66, No. 4Predictive Modeling of PROTAC Cell Permeability with Machine Learning1 February 2023 | ACS Omega, Vol. 8, No. 6Natural product-based PROteolysis TArgeting Chimeras (PROTACs)1 January 2022 | Natural Product Reports, Vol. 39, No. 12Linker-Dependent Folding Rationalizes PROTAC Cell Permeability28 September 2022 | Journal of Medicinal Chemistry, Vol. 65, No. 19Strategies for the discovery of oral PROTAC degraders aimed at cancer therapyCell Reports Physical Science, Vol. 3, No. 10The current state of the art and future trends in RAS-targeted cancer therapies26 August 2022 | Nature Reviews Clinical Oncology, Vol. 19, No. 10PROTACs: Current Trends in Protein Degradation by Proteolysis-Targeting Chimeras13 September 2022 | BioDrugs, Vol. 36, No. 5Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscopeActa Pharmaceutica Sinica B, Vol. 12, No. 7PROTAC targeted protein degraders: the past is prologue18 January 2022 | Nature Reviews Drug Discovery, Vol. 21, No. 3Hearing loss drug discovery and medicinal chemistry: Current status, challenges, and opportunities Vol. 14, No. 3 Follow us on social media for the latest updates Metrics Downloaded 1,804 times History Received 17 July 2021 Accepted 1 September 2021 Published online 29 September 2021 Published in print February 2022 Information© 2021 Newlands PressKeywordsADME/Toxdrug designin vitro assaysmolecular chameleonoral druggable spaceFinancial & competing interests disclosureThe authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.No writing assistance was utilized in the production of this manuscript.PDF download