| http://purl.uniprot.org/citations/16204896 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/16204896 | http://www.w3.org/2000/01/rdf-schema#comment | "Activated factor XI (FXIa) is a key enzyme in the amplification phase of the blood-coagulation cascade. Thus, a selective FXIa inhibitor may have lesser bleeding liabilities and provide a safe alternative for antithrombosis therapy to available drugs on the market. In a previous report, the crystal structures of the catalytic domain of FXIa (rhFXI(370-607)) in complex with various ecotin mutants have been described. However, ecotin forms a matrix-like interaction with rhFXI(370-607) and is impossible to displace with small-molecule inhibitors; ecotin crystals are therefore not suitable for iterative structure-based ligand design. In addition, rhFXI(370-607) did not crystallize in the presence of small-molecule ligands. In order to obtain the crystal structure of rhFXI(370-607) with a weak small-molecule ligand, namely benzamidine, several rounds of surface-residue mutation were implemented to promote crystal formation of rhFXI(370-607). A quadruple mutant of rhFXI(370-607) (rhFXI(370-607)-S434A,T475A,C482S,K437A) readily crystallized in the presence of benzamidine. The benzamidine in the preformed crystals was easily exchanged with other FXIa small-molecule inhibitors. These crystals have facilitated the structure-based design of small-molecule FXIa inhibitors."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.org/dc/terms/identifier | "doi:10.1107/s0907444905024340"xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/author | "Jin L."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/author | "Abdel-Meguid S.S."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/author | "Strickler J.E."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/author | "Pandey P."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/author | "Weaver D.T."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/author | "Babine R.E."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/date | "2005"xsd:gYear |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/name | "Acta Crystallogr D Biol Crystallogr"xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/pages | "1418-1425"xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/title | "Mutation of surface residues to promote crystallization of activated factor XI as a complex with benzamidine: an essential step for the iterative structure-based design of factor XI inhibitors."xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://purl.uniprot.org/core/volume | "61"xsd:string |
| http://purl.uniprot.org/citations/16204896 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/16204896 |
| http://purl.uniprot.org/citations/16204896 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/16204896 |
| http://purl.uniprot.org/uniprot/#_P03951-mappedCitation-16204896 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/16204896 |
| http://purl.uniprot.org/uniprot/P03951 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/16204896 |