Published in
Royal Society of Chemistry, Chemical Science, 46(10), p. 10789-10801, 2019
DOI: 10.1039/c9sc03445e
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Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S
Journal article published in 2019 by
Jonas Lategahn 
,
Marina Keul,
Philip Klövekorn,
Hannah L. Tumbrink,
Janina Niggenaber ,
Matthias P. Müller ,
Luke Hodson ,
Maren Flaßhoff,
Julia Hardick,
Tobias Grabe,
Julian Engel,
Carsten Schultz-Fademrecht,
Matthias Baumann,
Julia Ketzer,
Thomas Mühlenberg
and other authors.
,
Marina Keul,
Philip Klövekorn,
Hannah L. Tumbrink,
Janina Niggenaber ,
Matthias P. Müller ,
Luke Hodson ,
Maren Flaßhoff,
Julia Hardick,
Tobias Grabe,
Julian Engel,
Carsten Schultz-Fademrecht,
Matthias Baumann,
Julia Ketzer,
Thomas Mühlenberg
and other authors.
This paper is made freely available by the publisher.
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Abstract
We present inhibitors of drug resistant mutants of EGFR including T790M and C797S. In addition, we present the first X-ray crystal structures of covalent inhibitors in complex with C797S-mutated EGFR to gain insight into their binding mode.