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EGFR-T790M

Wednesday 4 April 2012

The T790M mutation was shown to confer resistance to gefitinib after it was introduced into the sequence of the wild-type EGFR and L858R mutant EGFR in vitro.

The T790M mutation results in steric hindrance of binding of gefitinib to the ATP-kinase–binding pocket.

References

- Detection of EGFR T790M mutation in plasma DNA from patients refractory to EGFR tyrosine kinase inhibitor. Sakai K, Horiike A, Irwin DL, Kudo K, Fujita Y, Tanimoto A, Sakatani T, Saito R, Kaburaki K, Yanagitani N, Ohyanagi F, Nishio M, Nishio K. Cancer Sci. 2013 May 31. doi : 10.1111/cas.12211 PMID: 23721103

- Challenges of detecting EGFR T790M in gefitinib/erlotinib-resistant tumours. Jänne PA. Lung Cancer. 2008 Jun;60 Suppl 2:S3-9. PMID: 18513582

- Screening for germline EGFR T790M mutations through lung cancer genotyping. Oxnard GR, Miller VA, Robson ME, Azzoli CG, Pao W, Ladanyi M, Arcila ME. J Thorac Oncol. 2012 Jun;7(6):1049-52. doi : 10.1097/JTO.0b013e318250ed9d PMID: 22588155