Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu)
A Reid, L Vidal, H Shaw, J de Bono - European journal of cancer, 2007 - Elsevier
… target inhibition on different receptors (Table 2)? This review will present the scientific rationale
for dual inhibition of … to date with a new generation of dual-targeting single-agent drugs. …
for dual inhibition of … to date with a new generation of dual-targeting single-agent drugs. …
Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity
F Montemurro, G Valabrega… - Expert opinion on …, 2007 - Taylor & Francis
… tyrosine kinase inhibitors, … inhibits the recombinant EGFR and HER2 tyrosine kinases by
50% (IC 50 ) at concentrations of 10.8 and 9.3 nmol/l, respectively. It acts as a reversible inhibitor…
50% (IC 50 ) at concentrations of 10.8 and 9.3 nmol/l, respectively. It acts as a reversible inhibitor…
Neratinib: an oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer
P Bose, H Ozer - Expert opinion on investigational drugs, 2009 - Taylor & Francis
… , dual reversible inhibitor of the EGFR and HER2 tyrosine kinases (TKs), was recently approved
by the FDA in combination with capecitabine for the treatment of HER2-… against HER2. …
by the FDA in combination with capecitabine for the treatment of HER2-… against HER2. …
Activity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitors
L Landi, M Tiseo, R Chiari, S Ricciardi, E Rossi… - Clinical lung cancer, 2014 - Elsevier
Background The purpose of this study was to evaluate the efficacy of afatinib in EGFR-mutant
metastatic NSCLC patients with acquired resistance to erlotinib or gefitinib. Materials and …
metastatic NSCLC patients with acquired resistance to erlotinib or gefitinib. Materials and …
Surmounting the resistance against EGFR inhibitors through the development of thieno [2, 3-d] pyrimidine-based dual EGFR/HER2 inhibitors
… through the development of dual EGFR/HER2 inhibitors with improved enzymatic affinities.
… dual EGFR/HER2 inhibitor, Lapatinib, we proposed the design of dual EGFR/HER2 inhibitors …
… dual EGFR/HER2 inhibitor, Lapatinib, we proposed the design of dual EGFR/HER2 inhibitors …
Therapeutic potential of the dual EGFR/HER2 inhibitor AZD8931 in circumventing endocrine resistance
G Morrison, X Fu, M Shea, S Nanda, M Giuliano… - Breast cancer research …, 2014 - Springer
… 72 h and downregulation of EGFR, HER2, and HER3 was detected … to EGFR and EGFR+HER2
inhibition. Both MCF7 and T47D TamRes cells were sensitive to EGFR and EGFR+HER2 …
inhibition. Both MCF7 and T47D TamRes cells were sensitive to EGFR and EGFR+HER2 …
EGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992
JF Spicer, SM Rudman - Targeted oncology, 2010 - Springer
… the potential of dual EGFR/HER2 inhibition. Lapatinib, a reversible EGFR/HER2 inhibitor,
has … Here we focus on BIBW 2992, a potent, irreversible inhibitor of both EGFR and HER2 …
has … Here we focus on BIBW 2992, a potent, irreversible inhibitor of both EGFR and HER2 …
Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in …
… , a small molecule tyrosine kinase inhibitor in a large panel of … HER2-amplified subgroup.
We provide a comparison between isolated EGFR inhibition with erlotinib and HER2 inhibition …
We provide a comparison between isolated EGFR inhibition with erlotinib and HER2 inhibition …
Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities–Part 1
D Das, L Xie, J Wang, X Xu, Z Zhang, J Shi, X Le… - Bioorganic & Medicinal …, 2019 - Elsevier
… 1), the second generation irreversible dual EGFR/HER2 inhibitor got approval by FDA for …
actively mutated EGFR. Erlotinib and gefitinib worked on EGFR and not worked on EGFR and …
actively mutated EGFR. Erlotinib and gefitinib worked on EGFR and not worked on EGFR and …
Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors
… HER2 notably with an IC 50 value of 2.28 ± 0.53 μM making it a dual EGFR and HER2 inhibitor.
… out that compound 3f showed high affinity into the ATP binding sites of EGFR and HER2. …
… out that compound 3f showed high affinity into the ATP binding sites of EGFR and HER2. …
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