| http://purl.uniprot.org/citations/25767113 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/25767113 | http://www.w3.org/2000/01/rdf-schema#comment | "The chemokine receptors CCR5 and CCR2b share 89% amino acid homology. CCR5 is a co-receptor for HIV and CCR5 antagonists have been investigated as inhibitors of HIV infection. We describe the use of two CCR5 antagonists, Schering-C (SCH-C), which is specific for CCR5, and TAK-779, a dual inhibitor of CCR5 and CCR2b, to probe the CCR5 inhibitor binding site using CCR5/CCR2b chimeric receptors. Compound inhibition in the different chimeras was assessed by inhibition of chemokine-induced calcium flux. SCH-C inhibited RANTES (regulated on activation, normal T cell expressed and secreted) (CCL5)-mediated calcium flux on CCR5 with an IC50 of 22.8 nM but was inactive against monocyte chemoattractant protein-1 (CCL2)-mediated calcium flux on CCR2b. However, SCH-C inhibited CCL2-induced calcium flux against a CCR5/CCR2b chimera consisting of transmembrane domains IV-VI of CCR5 with an IC50 of 55 nM. A sequence comparison of CCR5 and CCR2b identified a divergent amino acid sequence located at the junction of transmembrane domain V and second extracellular loop. Transfer of the CCR5 sequence KNFQTLKIV into CCR2b conferred SCH-C inhibition (IC50 of 122 nM) into the predominantly CCR2b chimera. Furthermore, a single substitution, R206I, conferred partial but significant inhibition (IC50 of 1023 nM) by SCH-C. These results show that a limited amino acid sequence is responsible for SCH-C specificity to CCR5, and we propose a model showing the interaction with CCR5 Ile(198)."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.org/dc/terms/identifier | "doi:10.1074/jbc.m115.640169"xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/author | "Labrecque J."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/author | "Metz M."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/author | "Lau G."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/author | "Vaz R."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/author | "Fricker S.P."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/date | "2015"xsd:gYear |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/name | "J Biol Chem"xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/pages | "11041-11051"xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/title | "Specificity for a CCR5 Inhibitor Is Conferred by a Single Amino Acid Residue: ROLE OF ILE198."xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://purl.uniprot.org/core/volume | "290"xsd:string |
| http://purl.uniprot.org/citations/25767113 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/25767113 |
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| http://purl.uniprot.org/uniprot/#_A0A089G6S6-mappedCitation-25767113 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/25767113 |
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| http://purl.uniprot.org/uniprot/#_A0A089G7G7-mappedCitation-25767113 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/25767113 |
| http://purl.uniprot.org/uniprot/#_A0A089G7G9-mappedCitation-25767113 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/25767113 |
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| http://purl.uniprot.org/uniprot/#_A0A089G3P4-mappedCitation-25767113 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/25767113 |