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Comment
. 2013 Sep 17;110(38):15169-70.
doi: 10.1073/pnas.1314719110. Epub 2013 Sep 10.

EGFR lung cancer mutants get specialized

Peter Littlefield  1 , Natalia Jura
Affiliations
Comment

EGFR lung cancer mutants get specialized

Peter Littlefield et al. Proc Natl Acad Sci U S A. .
No abstract available

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Fig. 1.
Fig. 1.
(A) Activation of EGFR receptors is dependent on asymmetric dimerization between the kinase domains. The donor kinase stabilizes the active conformation of the acceptor kinase through a set of hydrophobic interactions (magenta circle) between the N-lobe (N) of the acceptor kinase and the C-lobe (C) of the donor kinase. (B) When positioned as an acceptor kinase, NSCLC mutants L834R and L834R/T766M (“mut,” red star), result in more efficient signaling than wild-type (WT) EGFR. However, NSCLC mutants fail to serve as donor kinases. (C) Monomeric EGFR kinase is primarily inactive because of the occlusion of the activator interface (magenta) within the N-lobe. Activating mutations in the acceptor kinase promote dimerization through partial destabilization of the inactive conformation.
See this image and copyright information in PMC

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