| http://purl.uniprot.org/citations/18287036 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/18287036 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/18287036 | http://www.w3.org/2000/01/rdf-schema#comment | "Analysis of the x-ray crystal structure of mono-substituted acetylenic thienopyrimidine 6 complexed with the ErbB family enzyme ErbB-4 revealed a covalent bond between the terminal carbon of the acetylene moiety and the sulfhydryl group of Cys-803 at the solvent interface. The identification of this covalent adduct suggested that acetylenic thienopyrimidine 6 and related analogs might also be capable of forming an analogous covalent adduct with EGFR, which has a conserved cysteine (797) near the ATP binding pocket. To test this hypothesis, we treated a truncated, catalytically competent form of EGFR (678-1020) with a structurally related propargylic amine (8). An investigation of the resulting complex by mass spectrometry revealed the formation of a covalent complex of thienopyrimidine 8 with Cys-797 of EGFR. This finding enabled us to readily assess the irreversibility of various inhibitors and also facilitated a structure-activity relationship understanding of the covalent modifying potential and biological activity of a series of acetylenic thienopyrimidine compounds with potent antitumor activity. Several ErbB family enzyme and cell potent 6-ethynyl thienopyrimidine kinase inhibitors were found to form covalent adducts with EGFR."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.org/dc/terms/identifier | "doi:10.1073/pnas.0708281105"xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.org/dc/terms/identifier | "doi:10.1073/pnas.0708281105"xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Vanderwall D.E."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Vanderwall D.E."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Ellis B."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Ellis B."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Williams J.D."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Williams J.D."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Keith B."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Keith B."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Wood E.R."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Wood E.R."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Shewchuk L.M."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Shewchuk L.M."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Uehling D.E."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Uehling D.E."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Hassell A.M."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Hassell A.M."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Dickerson S.H."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Dickerson S.H."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Rusnak D.W."xsd:string |
| http://purl.uniprot.org/citations/18287036 | http://purl.uniprot.org/core/author | "Rusnak D.W."xsd:string |