Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.

By E. Kwak, Raffaella Sordella, D. Bell, N. Godin-Heymann, R. Okimoto, Brian W. Brannigan, Patricia L. Harris, David R. Driscoll, P. Fidias, T. Lynch and 7 more. Proceedings of the National Academy of Sciences of the United States of America, 2005

972 citations recorded by the source corpus.

Subfields: Genetics, Oncology, Pulmonary and Respiratory Medicine

View Paper: https://www.semanticscholar.org/paper/1bc0f4db096320ac34abed2404a5bfb66311af72

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Genetics

1. J. Engelman

In Oncology

1. J. Engelman
2. Jin-Yuan Shih
3. Shang-Gin Wu
4. P. Jänne
5. G. Shapiro
6. James E. Bradner

In Pulmonary and Respiratory Medicine

1. Jin-Yuan Shih
2. J. Engelman
3. Shang-Gin Wu
4. P. Jänne
5. James E. Bradner

Citations in the corpus

• The resurgence of covalent drugs (2011, background): “It appears that irreversible inhibitors may maintain activity against drug-resistant mutations that are acquired after treatment with reversible inhibitor”
• Acquired resistance to EGFR tyrosine kinase inhibitors in EGFR mutant lung cancer: Distinct natural history of patients with tumors harboring the T790M mutation (2010, neutral): “Median time from progression to new metastatic organ involvement, months* 14 (8-18) 4 (1-9) 0.”
• Liquid biopsy: a step closer to transform diagnosis, prognosis and future of cancer treatments (2022, background): “Interestingly, such mutations may positively predict therapeutic responses against newer irreversible EGFR tyrosine kinase inhibitors [76].”
• The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP (2008, background): “The irreversible inhibitor HKI-272 is a 4-(arylamino)quinoline-3-carbonitrile compound and a potent inhibitor of both EGFR and ErbB2 kinases (14, 30).”