RDF/XMLNTriplesTurtleShow queryShare
SubjectPredicateObject
http://purl.uniprot.org/citations/20103630http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/20103630http://www.w3.org/2000/01/rdf-schema#comment"Ongoing clinical trials are exploring anticancer approaches based on signaling by TRAIL, a ligand for the cell death receptors DR4 and DR5. In this study, we report on the selective apoptotic effects of multivalent DR5 binding peptides (TRAIL(mim/DR5)) on cancer cells in vitro and in vivo. Surface plasmon resonance revealed up to several thousand-fold increased affinities of TRAIL(mim/DR5)-receptor complexes on generation of divalent and trivalent molecules, the latter of which was achieved with a conformationally restricted adamantane core. Notably, only multivalent molecules triggered a substantial DR5-dependent apoptotic response in vitro. In tumor models derived from human embryonic kidney cells or primary foreskin fibroblasts, TRAIL(mim/DR5) peptides exerted a cancer cell-selective action that could synergize with resveratrol in a manner independent of p53. In a xenograft model of human colon cancer, a divalent TRAIL(mim/DR5) peptide inhibited tumor growth. Our results offer a proof-of-principle for the development of synthetic small molecules to trigger the TRAIL apoptosis pathway for cancer therapy."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.org/dc/terms/identifier"doi:10.1158/0008-5472.can-09-2889"xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Guichard G."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Wendland M."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Micheau O."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Pardin C."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Pavet V."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Fournel S."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Lechner M.C."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Gronemeyer H."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Briand J.P."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Beyrath J."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Morizot A."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/author"Maison W."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/date"2010"xsd:gYear
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/name"Cancer Res"xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/pages"1101-1110"xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/title"Multivalent DR5 peptides activate the TRAIL death pathway and exert tumoricidal activity."xsd:string
http://purl.uniprot.org/citations/20103630http://purl.uniprot.org/core/volume"70"xsd:string
http://purl.uniprot.org/citations/20103630http://www.w3.org/2004/02/skos/core#exactMatchhttp://purl.uniprot.org/pubmed/20103630
http://purl.uniprot.org/citations/20103630http://xmlns.com/foaf/0.1/primaryTopicOfhttps://pubmed.ncbi.nlm.nih.gov/20103630
http://purl.uniprot.org/uniprot/#_O14763-mappedCitation-20103630http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/20103630
http://purl.uniprot.org/uniprot/#_O14798-mappedCitation-20103630http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/20103630
http://purl.uniprot.org/uniprot/#_Q13158-mappedCitation-20103630http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/20103630