{"doi":"10.1006/excr.1997.3616","title":"Selective Inhibition of Platelet-Derived Growth Factor (PDGF) Receptor Autophosphorylation and PDGF-Mediated Cellular Events by a Quinoline Derivative","abstract":null,"journal":"Experimental Cell Research","year":1997,"id":663299,"datarank":0.42498200160843247,"base_score":2.833213344056216,"endowment":2.833213344056216,"self_citation_contribution":0.42498200160843247,"citation_network_contribution":0.0,"self_endowment_contribution":0.42498200160843247,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":16,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":306535,"name":"Shinichiro Kato","orcid":null,"position":1,"is_corresponding":false},{"id":1731729,"name":"Yoshiko Kobayashi","orcid":null,"position":2,"is_corresponding":false},{"id":1731730,"name":"Kazuo Kubo","orcid":null,"position":3,"is_corresponding":false},{"id":1731731,"name":"Shinichi Oyama","orcid":null,"position":4,"is_corresponding":false},{"id":126883,"name":"Toshiyuki Shimizu","orcid":null,"position":5,"is_corresponding":false},{"id":1731732,"name":"Tsuyoshi Nishitoba","orcid":null,"position":6,"is_corresponding":false},{"id":1731733,"name":"Toshiyuki Isoe","orcid":null,"position":7,"is_corresponding":false},{"id":1731734,"name":"Kazuhide Nakamura","orcid":null,"position":8,"is_corresponding":false},{"id":1731735,"name":"Hideya Ohashi","orcid":null,"position":9,"is_corresponding":false},{"id":1731736,"name":"Nami Kobayashi","orcid":null,"position":10,"is_corresponding":false},{"id":1731737,"name":"Noriko Iinuma","orcid":null,"position":11,"is_corresponding":false},{"id":1731738,"name":"Tatsushi Osawa","orcid":null,"position":12,"is_corresponding":false},{"id":1731739,"name":"Rie Onose","orcid":null,"position":13,"is_corresponding":false},{"id":812350,"name":"Hiroyuki Osada","orcid":"0000-0002-3606-4925","position":14,"is_corresponding":false},{"id":1731728,"name":"Mikio Yagi","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Selective Inhibition of Platelet-Derived Growth Factor (PDGF) Receptor Autophosphorylation and PDGF-Mediated Cellular Events by a Quinoline Derivative","abstract":"This report describes the biological effects of our original compound, Ki6783 ((3,4-dimethoxy)-4-phenoxy-6,7-dimethoxyquinoline), a potent and selective inhibitor of platelet-derived growth factor (PDGF) receptor autophosphorylation. This compound strongly inhibited autophosphorylation of the PDGF beta-receptor in cultured rat glomerular mesangial cells (MC) bearing this receptor (IC50 0.1 microM), although it did not inhibit autophosphorylation of other growth factor receptors even at 100 microM. In a cell-free kinase experiment, it showed selective inhibition of PDGF beta-receptor tyrosine kinase. A kinetic study of the compound to this tyrosine kinase revealed a competitive mode of action to ATP. [3H]Thymidine incorporation and cell proliferation of MC were inhibited by Ki6783 in a dose-dependent manner after Ki6783 and PDGF-BB were added to the culture medium. Furthermore, this compound normalized the fibrotic cell shape of v-sis-transformed NIH3T3 cells, which grow in an autocrine manner via the PDGF receptor. These effects could be explained by the inhibition of intracellular signal transduction triggered by PDGF receptor autophosphorylation, in which activation of mitogen-activated protein kinase occurs. These results suggest that Ki6783 is one of the more potent and selective inhibitors of PDGF receptor autophosphorylation and that it may be useful in ameliorating cell abnormalities due to excess action of PDGF and its receptor systems in several diseases.","is_dataset_classified":null,"base_score":2.833213344056216,"endowment":2.833213344056216,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"9260896","pmcid":null,"openalex_id":"https://openalex.org/W2042649794","authors":[],"funders":[],"total_grants":0,"fwci":0.8527,"citation_percentile":0.7262221,"influential_citations":0,"citation_trend":[{"year":2014,"count":1}],"oa_status":"closed","license":"https://www.elsevier.com/tdm/userlicense/1.0/","oa_locations":[{"url":"https://api.elsevier.com/content/article/PII:S0014482797936168?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0014482797936168?httpAccept=text/plain","host_type":"publisher"},{"url":"https://doi.org/10.1006/excr.1997.3616","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/9260896","host_type":"repository"}],"fields_of_study":["PI3K/AKT/mTOR signaling in cancer","Protein Tyrosine Phosphatases","Protein Kinase Regulation and GTPase Signaling","3T3 Cells","Adenosine Triphosphate","Animals","Becaplermin","Calcium-Calmodulin-Dependent Protein Kinases","Cell Division","Cell Line, Transformed","Cell Size","Cells, Cultured","DNA","Enzyme Activation","Enzyme Inhibitors","Glomerular Mesangium","Humans","Kinetics","Male","Mice","Phosphorylation","Platelet-Derived Growth Factor","Proto-Oncogene Proteins c-sis","Quinolines","Rats","Rats, Inbred WKY","Receptor Protein-Tyrosine Kinases","Receptor, Platelet-Derived Growth Factor beta","Receptors, Platelet-Derived Growth Factor","Signal Transduction"],"mesh_terms":["Becaplermin","Adenosine Triphosphate","Animals","Cell Division","Cell Line, Transformed","Cells, Cultured","DNA","Enzyme Activation","Enzyme Inhibitors","Glomerular Mesangium","Humans","Kinetics","Male","Phosphorylation","Platelet-Derived Growth Factor","Quinolines","Rats, Inbred WKY","Signal Transduction","3T3 Cells","Receptors, Platelet-Derived Growth Factor","Calcium-Calmodulin-Dependent Protein Kinases","Proto-Oncogene Proteins c-sis","Receptor Protein-Tyrosine Kinases","Receptor, Platelet-Derived Growth Factor beta","Cell Size","Mice","Rats"],"keywords":["Autophosphorylation","Platelet-derived growth factor receptor","Biology","Platelet-derived growth factor","Quinoline","Growth factor","Growth factor receptor","Cell biology","Receptor","Cancer research","Biochemistry","Pharmacology","Phosphorylation","Signal transduction","Protein kinase A","Chemistry"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-12T21:02:04.108021Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}