EGFR receptors- missing lecture Flashcards
____ cancers overexpress HER2 than EGFR
fewer
small molecule EGFR approaches?
gefitinib
erlotinib
mAb approaches to EGFR
Cetuximab
panitumumab
cetuximab is commonly used in ______ therapy with?
combination
radiotherapy
what can reduce the effectiveness of EGFR inhibitors
if theyre K-RAS mutant
what happens in K-RAS mutations?
it stops the feedthrough at the receptor so the EGFR drug doesn’t have an effect
active despite whats happening upstream
what is cetuximab lisenced for treatment in?
bowel cancer
head and neck cancer
what do patients need to be screened for prior to recieving cetuximab?
K-Ras mutation
which patients respond well to small molecule EGFR inhibitors?
mutated EGFR
Is simple over-expression of EGFR enough to tell us if the patient will respond to a small molecule inhibitor?
no
why does mutated EGFR show an increased response to blocking?
as the tumour becomes reliant on the increased EGFR signalling so blocking this shows good results
major differences between mutated and wild type EGFR:
regarding 1. activation
wild type is activated by ligands (homodimerisation and autophosphorylation)
mutant can be active in the absence of the lingand
major differences between mutated and wild type EGFR:
regarding 1. Pathways/ signalling cascades
enhanced with mutant EGFR
major differences between mutated and wild type EGFR:
regarding 1. sensitivity to TKI’s?
context dependent in wild type but the mutant EGFR is sensitised
major differences between mutated and wild type EGFR:
regarding 1. Ubiquitin mediated degradation
ubiquitin- mediated degradation of wild ytpe EGFR is ligand induced
mutant EGFR shows elevated ubiquitinylation
