References
- 1. . Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: recent progress and future challenges. Bioorg. Med. Chem. Lett. 29, 1555–1564 (2019).
- 2. . Developing degraders: principles and perspectives on design and chemical space. Med. Chem. Commun. 10, 1755–1764 (2019).
- 3. . Oral druggable space beyond the rule of 5: insights from drugs and clinical candidates. Chem. Biol. 21, 1115–1142 (2014).
- 4. . Beyond the rule of 5: lessons learned from AbbVie's drugs and compound collection. J. Med. Chem. 61, 2636–2651 (2018).
- 5. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 46, D1074–D1082 (2018).
- 6. PROTAC-DB: an online database of PROTACs. Nucleic Acids Res. 49(D1), D1381–D1387 (2021).
- 7. Solution conformations shed light on PROTAC cell permeability. ACS Med. Chem. Lett. 12, 107–114 (2021).
- 8. . Solution conformations explain the chameleonic behavior of macrocyclic drugs. Chem. Eur. J. 26(23), 5231–5244 (2020).
- 9. Understanding and improving the membrane permeability of VH032-based PROTACs. ACS Med. Chem. Lett. 11(9), 1732–1738 (2020).
- 10. . Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective. Drug Discov. Today 25, 1793-1800 (2020).
- 11. . Fundamental aspects of DMPK optimization of targeted protein degraders. Drug Discov. Today 25, 969–982 (2020).
- 12. . Degraders early developability assessment: face-to-face with molecular properties. Drug Discov. Today 25(9), 1585–1591 (2020).
- 13. Systematic investigation of the permeability of androgen receptor PROTACs. ACS Med. Chem. Lett. 11, 1539–1547 (2020).
- 14. . Arvinas unveils PROTAC structures. Chem. Eng. News 99(14), magazine/99/09914 (2021).
- 15. A chemical approach for global protein knockdown from mice to non-human primates. Cell Discov. 5, 10 (2019).
- 16. PROTAC-mediated degradation of Bruton's tyrosine kinase is inhibited by covalent binding. ACS Chem. Biol. 14, 342–347 (2019).
- 17. Conformational sampling of macrocyclic drugs in different environments – can we find the relevant conformations? ACS Omega 3, 11742–11757 (2018).
- 18. Predicting the permeability of macrocycles from conformational sampling – limitations of molecular flexibility. J. Pharm. Sci. 110, 301–313 (2021).
- 19. . Understanding the metabolism of proteolysis targeting chimeras (PROTACs): the next step toward pharmaceutical applications. J. Med. Chem. 63, 11615–11638 (2020).
- 20. . Unraveling the role of linker design in proteolysis targeting chimeras. J. Med. Chem. 64, 8042–8052 (2021).