[HTML][HTML] The epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor AG1478 increases the formation of inactive untethered EGFR dimers: implications for …

HK Gan, F Walker, AW Burgess, A Rigopoulos… - Journal of biological …, 2007 - ASBMB
The epidermal growth factor receptor (EGFR) has at least two fundamental conformations:
an inactive tethered conformation and an active untethered, ligand-bound" back-toback"
dimer, which may be part of an oligomeric complex. Monoclonal antibody (mAb) 806 is an
EGFR-specific antibody that only binds a transitional form of the receptor after it untethers
but before forming the back-to-back, ligated, active oligomer. We have shown that AG1478,
a tyrosine kinase inhibitor of the EGFR, synergistically inhibits the growth of tumors …