Publications by authors named "Maaike Emmelot"
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.
Bioorg Med Chem Lett
November 2021
Article Synopsis
- EGFR inhibitors effectively treat non-small cell lung cancer (NSCLC), but many patients develop resistance, mainly due to the T790M mutation, often alongside L858R.
- Resistance to these treatments leads to disease progression, and EGFR wild type inhibition can cause significant side effects like rash and diarrhea.
- A new compound, lead 12, has been identified as a selective irreversible inhibitor that targets the T790M and L858R mutations without affecting the wild type EGFR, showing promising tumor growth inhibition in preclinical studies.