Design, synthesis and biological evaluation of erlotinib-based IDO1 inhibitors
Erlotinib is a highly specific and reversible epidermal growth factor receptor tyrosine kinase inhibitor for the targeted therapy of non-small-cell lung cancer (NSCLC) However, the efficacy of erlotinib is limited because the development of drug ...
Xi-xi Hou +6 more
doaj +1 more source
Erlotinib is a viable treatment for tumors with acquired resistance to cetuximab [PDF]
The epidermal growth factor receptor (EGFR) is a ubiquitously expressed receptor tyrosine kinase (RTK) and is recognized as a key mediator of tumorigenesis in many human tumors. Currently there are five EGFR inhibitors used in oncology, two monoclonal antibodies (panitumumab, and cetuximab) and three tyrosine kinase inhibitors (erlotinib, gefitinib ...
Toni M, Brand +7 more
openaire +2 more sources
EGFR signaling promotes ovarian cancer tumorigenesis, and high EGFR expression correlates with poor prognosis. However, EGFR inhibitors alone have demonstrated limited clinical benefit for ovarian cancer patients, owing partly to tumor resistance and the
Victor CY Mak +5 more
doaj +1 more source
Transcriptomic-metabolomic reprogramming in EGFR-mutant NSCLC early adaptive drug escape linking TGFβ2-bioenergetics-mitochondrial priming. [PDF]
The impact of EGFR-mutant NSCLC precision therapy is limited by acquired resistance despite initial excellent response. Classic studies of EGFR-mutant clinical resistance to precision therapy were based on tumor rebiopsies late during clinical tumor ...
Bagai, Rakesh +14 more
core +1 more source
GRHL2-HER3 and E-cadherin mediate EGFR-bypass drug resistance in lung cancer cells
Epidermal growth factor receptor (EGFR) is a major oncogenic protein, and thus EGFR-targeting therapies are widely used in patients with various types of cancer, including lung cancer. However, resistance to EGFR inhibitors, such as erlotinib, presents a
Fumiya Ito +4 more
doaj +1 more source
Erlotinib, an EGFR tyrosine kinase inhibitor, is used for treating patients with cancer exhibiting EGFR overexpression or mutation. However, the response rate of erlotinib is low among patients with gastric cancer (GC).
Fangyuan Li +17 more
doaj +1 more source
Differential responsiveness of MET inhibition in non-small-cell lung cancer with altered CBL. [PDF]
Casitas B-lineage lymphoma (CBL) is an E3 ubiquitin ligase and a molecule of adaptor that we have shown is important for non-small-cell lung cancer (NSCLC). We investigated if MET is a target of CBL and if enhanced in CBL-altered NSCLC.
Batra, Surinder K +9 more
core +1 more source
A phase Ib/II study of cabozantinib (XL184) with or without erlotinib in patients with non-small cell lung cancer. [PDF]
PurposeCabozantinib is a multi-kinase inhibitor that targets MET, AXL, and VEGFR2, and may synergize with EGFR inhibition in NSCLC. Cabozantinib was assessed alone or in combination with erlotinib in patients with progressive NSCLC and EGFR mutations who
Engelman, Jeffrey +10 more
core +2 more sources
Human lung adenocarcinoma cell cultures derived from malignant pleural effusions as model system to predict patients chemosensitivity [PDF]
BACKGROUND: Lung cancer is the leading cause of cancer related deaths and Malignant Pleural Effusion (MPE) is a frequent complication. Current therapies suffer from lack of efficacy in a great percentage of cases, especially when cancer is diagnosed at ...
CHERUBINI, EMANUELA +17 more
core +3 more sources
Substrate‐dependent bidirectional modulation of P‐glycoprotein‐mediated drug resistance by erlotinib [PDF]
Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR‐TKIs) inhibit the function of certain adenosine triphosphate (ATP)‐binding cassette transporters, including P‐glycoprotein/ABCB1 and breast cancer resistance protein (BCRP)/ABCG2. We previously reported an antagonistic activity of gefitinib towards BCRP.
Kohji, Noguchi +5 more
openaire +2 more sources

