Exploiting intracellular oncogenic proteins to release cytotoxins
Abstract
-cyclooctene (TCO) caged prodrugs. This concept was demonstrated using the epidermal growth factor receptor (EGFR), a key therapeutic target in non-small cell lung cancer. An afatinib-tetrazine conjugate achieved sufficient intracellular retention in EGFR-overexpressing cells to enable toxicity recovery from a TCO-protected monomethyl auristatin E (MMAE) derivative. Successful intracellular targeting and controlled payload release establish a foundation for expanding the scope of targeted drug delivery to previously inaccessible oncogenic drivers.
Fields of Study & Subjects
HER2/EGFR in Cancer Research
Monoclonal and Polyclonal Antibodies Research
Click Chemistry and Applications
Publication details
- Journal / source
- RSC Medicinal Chemistry
- Publisher
- Royal Society of Chemistry (RSC)
- Volume
- 17
- Issue
- 2
- Pages
- 1155–1165
- Publication date
- 1 January 2026
- Language
- EN