Anti-EGFR Therapy: Mechanism and Advances in Clinical Efficacy in Breast Cancer
Figure 3
Molecular and crystal structures of EGFR
inhibitor Lapatinib and Lapatinib bound and complexed to EGFR
ATP-binding pocket, respectively. (a) Molecular
structure of Lapatinib (CID208908), an EGFR-ErbB2 inhibitor. (b) Overlay
of EGFR in the Lapatinib and Erlotinib complexes. EGFR in the Lapatinib and Erlotinib structures
is shown as red and green ribbons, respectively. Lapatinib is shown as a yellow
space-filling model. The two proteins were overlaid based on residues in the
COOH-terminal domain of the kinase. The COOH-terminal in both structures is CT.
Disordered residues in the COOH-terminal tail of EGFR are indicated by a dashed
line. The figure was prepared using QUANTA (Accelrys), adapted from Wood et al.
[36].
