http://purl.uniprot.org/citations/22431598 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/22431598 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/22431598 | http://www.w3.org/2000/01/rdf-schema#comment | "The Ras gene is frequently mutated in cancer, and mutant Ras drives tumorigenesis. Although Ras is a central oncogene, small molecules that bind to Ras in a well-defined manner and exert inhibitory effects have not been uncovered to date. Through an NMR-based fragment screen, we identified a group of small molecules that all bind to a common site on Ras. High-resolution cocrystal structures delineated a unique ligand-binding pocket on the Ras protein that is adjacent to the switch I/II regions and can be expanded upon compound binding. Structure analysis predicts that compound-binding interferes with the Ras/SOS interactions. Indeed, selected compounds inhibit SOS-mediated nucleotide exchange and prevent Ras activation by blocking the formation of intermediates of the exchange reaction. The discovery of a small-molecule binding pocket on Ras with functional significance provides a new direction in the search of therapeutically effective inhibitors of the Ras oncoprotein."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.org/dc/terms/identifier | "doi:10.1073/pnas.1116510109"xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.org/dc/terms/identifier | "doi:10.1073/pnas.1116510109"xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Fang G."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Fang G."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Wu J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Wu J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Wang W."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Wang W."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Rudolph J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Rudolph J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Pan B."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Pan B."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Jackson P.K."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Jackson P.K."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Stokoe D."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Stokoe D."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Anderson D.J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Anderson D.J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Skelton N.J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Skelton N.J."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Mellman I."xsd:string |
http://purl.uniprot.org/citations/22431598 | http://purl.uniprot.org/core/author | "Mellman I."xsd:string |