{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["9(30)"],"submitter":["Yu CH"],"pubmed_abstract":["Afatinib, used for the first-line treatment of non-small-cell lung carcinoma (NSCLC) patients with distinct epidermal growth factor receptor (EGFR) mutations, inactivates EGFR by mimicking ATP structure and forming a covalent adduct with EGFR. We developed a method to unravel potential targets of afatinib in NSCLC cells through immunoprecipitation of afatinib-labeling proteins with anti-afatinib antiserum and mass spectrometry analysis. Ribonucleotide reductase (RNR) is one of target proteins of afatinib revealed by this method. Treatment of afatinib at 10-100 nM potently inhibited intracellular RNR activity in an <i>in vitro</i> assay using permeabilized PC-9 cells (formerly known as PC-14). PC-9 cells treated with 10 μM afatinib displayed elevated markers of DNA damage. Long-term treatme"],"journal":["Oncotarget"],"pagination":["21512-21529"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5940374"],"repository":["biostudies-literature"],"pubmed_title":["Antibody-assisted target identification reveals afatinib, an EGFR covalent inhibitor, down-regulating ribonucleotide reductase."],"pmcid":["PMC5940374"],"pubmed_authors":["Ho YY","Yu CH","Chang GD","Lee MS","Tu HF","Khoo KH","Chou CC","Huang WC"],"additional_accession":[]},"is_claimable":false,"name":"Antibody-assisted target identification reveals afatinib, an EGFR covalent inhibitor, down-regulating ribonucleotide reductase.","description":"Afatinib, used for the first-line treatment of non-small-cell lung carcinoma (NSCLC) patients with distinct epidermal growth factor receptor (EGFR) mutations, inactivates EGFR by mimicking ATP structure and forming a covalent adduct with EGFR. We developed a method to unravel potential targets of afatinib in NSCLC cells through immunoprecipitation of afatinib-labeling proteins with anti-afatinib antiserum and mass spectrometry analysis. Ribonucleotide reductase (RNR) is one of target proteins of afatinib revealed by this method. Treatment of afatinib at 10-100 nM potently inhibited intracellular RNR activity in an <i>in vitro</i> assay using permeabilized PC-9 cells (formerly known as PC-14). PC-9 cells treated with 10 μM afatinib displayed elevated markers of DNA damage. Long-term treatme","dates":{"release":"2018-01-01T00:00:00Z","publication":"2018 Apr","modification":"2026-05-04T22:59:36.922Z","creation":"2019-03-26T23:37:41Z"},"accession":"S-EPMC5940374","cross_references":{"pubmed":["29765556"],"doi":["10.18632/oncotarget.25177"]}}