The Panitumumab EGFR Complex Reveals a Binding Mechanism That Overcomes Cetuximab Induced Resistance.
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ABSTRACT:
SUBMITTER: Sickmier EA
PROVIDER: S-EPMC5033319 | biostudies-literature | 2016
REPOSITORIES: biostudies-literature
Publications
The Panitumumab EGFR Complex Reveals a Binding Mechanism That Overcomes Cetuximab Induced Resistance.
Sickmier E Allen EA Kurzeja Robert J M RJ Michelsen Klaus K Vazir Mukta M Yang Evelyn E Tasker Andrew S AS
PloS one 20160922 9
Panitumumab and cetuximab target the epidermal growth factor receptor for the treatment of metastatic colorectal cancer. These therapies provide a significant survival benefit to patients with metastatic colorectal cancer with wild-type RAS. A single point mutation in the ectodomain of EGFR (S468R) confers acquired or secondary resistance in cetuximab treated patients, which is not observed in panitumumab-treated patients. Structural and biophysical studies presented here show this mutation dire ...[more]
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