EGFR‐HER2 Transactivation Viewed in Space and Time Through the Versatile Spectacles of Imaging Cytometry—Implications for Targeted Therapy
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DOI: 10.1002/cyto.a.24922
Abstract: Ligand‐induced formation of signaling platforms composed of homo‐ and/or heterodimers of receptor tyrosine kinases is considered essential for their activation and consequential contribution to the progression of many cancers. Epidermal Growth Factor Receptor (EGFR) acts… read more here.
Keywords: receptor; time; her2; transactivation ... See more keywords
TMEM16A/ANO1 suppression improves response to antibody‐mediated targeted therapy of EGFR and HER2/ERBB2
Sign Up to like & getrecommendations! Published in 2017 at "Genes"
DOI: 10.1002/gcc.22450
Abstract: TMEM16A, a Ca2+‐activated Cl− channel, contributes to tumor growth in breast cancer and head and neck squamous cell carcinoma (HNSCC). Here, we investigated whether TMEM16A influences the response to EGFR/HER family‐targeting biological therapies. Inhibition of… read more here.
Keywords: egfr her2; improves response; tmem16a; antibody ... See more keywords
Rapid screening of drug candidates against EGFR/HER2 signaling pathway using fluorescence assay
Sign Up to like & getrecommendations! Published in 2018 at "Analytical and Bioanalytical Chemistry"
DOI: 10.1007/s00216-018-1403-1
Abstract: AbstractOver the recent decade, the calcium-based assays have gained much popularity in order to discover new drugs. Since breast cancer is the second cause of death in the female population, rapid and effective methods are… read more here.
Keywords: fluorescence; drug candidates; signaling pathway; egfr her2 ... See more keywords
Dual EGFR/HER2 inhibitors and apoptosis inducers: New benzo[g]quinazoline derivatives bearing benzenesulfonamide as anticancer and radiosensitizers.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.07.015
Abstract: Dual targeting of EGFR and HER2 is a proven anticancer strategy for the treatment of solid tumors. An array of new N-substituted-2-(4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydrobenzo[g]quinazolin-2-ylthio) acetamides 5-18 were designed and synthesized from the starting compound 4-(2-mercapto-4-oxobenzo[g]quinazolin-3(4H)-yl) benzenesulfonamide 4.… read more here.
Keywords: dual egfr; her2 inhibitors; anticancer; egfr her2 ... See more keywords
Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR/HER2.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103461
Abstract: We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward cancer… read more here.
Keywords: cytotoxic; ic50; egfr her2; activity ... See more keywords
Design, synthesis and anticancer evaluation of new 4-anilinoquinoline-3-carbonitrile derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers.
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DOI: 10.1016/j.bioorg.2021.105200
Abstract: Dual targeting of EGFR/HER2 receptor is an attractive strategy for cancer therapy. Four series of 4-anilinoquinoline-3-carbonitrile derivatives were designed and prepared by introducing various functional groups, including a polar hydrophilic group (carboxylic acid), a heterocyclic… read more here.
Keywords: her2; carbonitrile derivatives; egfr her2; anticancer ... See more keywords
Inhibition of glycolysis by a novel EGFR/HER2 inhibitor KU004 suppresses the growth of HER2+ cancer
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DOI: 10.1016/j.yexcr.2017.05.019
Abstract: &NA; Upregulation of glycolysis was often observed in human HER2‐overexpressing cancers. In this study, we demonstrated that KU004, a dual novel EGFR/HER2 inhibitor, disrupted cancer cell proliferation via modulation of glycolysis. KU004, inhibited the Warburg… read more here.
Keywords: egfr her2; ku004; glycolysis; novel egfr ... See more keywords
Harnessing Machine Learning for the Virtual Screening of Natural Compounds as Both EGFR and HER2 Inhibitors in Colorectal Cancer: A Novel Therapeutic Approach
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DOI: 10.1021/acsomega.5c07683
Abstract: Colorectal cancer (CRC) is a type of cancer that affects the colon and rectum, with overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) observed in up to 85%… read more here.
Keywords: colorectal cancer; cancer; her2 inhibitors; machine learning ... See more keywords
A Correlative Analysis of PD-L1, PD-1, PD-L2, EGFR, HER2, and HER3 Expression in Oropharyngeal Squamous Cell Carcinoma
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DOI: 10.1158/1535-7163.mct-17-0504
Abstract: We explored potential associations of the PD-1/PD-L1/PD-L2 pathway with clinical characteristics, outcome, and expression of EGFR, HER2, HER3 in oropharyngeal squamous cell carcinoma (OPSCC) using an institutional database. Protein expression was assessed by IHC on… read more here.
Keywords: egfr her2; her2 her3; expression;
Abstract 1824: Mechanisms of resistance to anti-EGFR/HER2 therapy in breast cancer
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DOI: 10.1158/1538-7445.am2018-1824
Abstract: Therapy resistance to epidermal growth factor receptor family (EGFR and HER2) targeted therapies has been an obstacle for treatment success in breast cancer. Therefore, our goal is to investigate the mechanisms of resistance to these… read more here.
Keywords: therapy; egfr her2; resistance; breast cancer ... See more keywords
Abstract CT126: An open-label, first-in-human study of BAY2927088 in patients with advanced non-small cell lung cancer (NSCLC) harboring an EGFR and/or HER2 mutation
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-ct126
Abstract: Background: Despite targeted agents recently approved for treating patients with advanced NSCLC harboring EGFR exon 20 insertion (ex20ins) mutations, there is still a high unmet need for more effective agents with good tolerability. BAY2927088 is… read more here.
Keywords: nsclc harboring; patients advanced; bay2927088; egfr her2 ... See more keywords