Structure–Activity Relationship Study of Cyclic Pentapeptide Ligands for Atypical Chemokine Receptor 3 (ACKR3)
| Autor: | Tomoko Kuroyanagi, Yuka Kobayashi, Hiroaki Ohno, Nobutaka Fujii, Kenichi Akaji, David Rhainds, Shinya Oishi, Nikolaus Heveker, Kazuya Kobayashi, Haruka Sekiguchi |
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| Rok vydání: | 2018 |
| Předmět: |
Models
Molecular 0301 basic medicine Stromal cell Stereochemistry Ligands Peptides Cyclic Structure-Activity Relationship 03 medical and health sciences Chemokine receptor 0302 clinical medicine Drug Discovery Side chain Humans Structure–activity relationship CXC chemokine receptors Receptors CXCR chemistry.chemical_classification Molecular Structure Chemistry Ligand 3. Good health Amino acid HEK293 Cells 030104 developmental biology Amino Acid Substitution 030220 oncology & carcinogenesis Molecular Medicine Cyclic pentapeptide |
| Zdroj: | Journal of Medicinal Chemistry. 61:3745-3751 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/acs.jmedchem.8b00336 |
| Popis: | The atypical chemokine receptor 3 (ACKR3)/CXC chemokine receptor 7 (CXCR7) recognizes stromal cell-derived factor 1 (SDF-1)/CXCL12 and is involved in a number of physiological and pathological processes. Here, we investigated the SAR of the component amino acids in an ACKR3-selective ligand, FC313 [ cyclo(-d-Tyr-l-Arg-l-MeArg-l-Nal(2)-l-Pro-)], for the development of highly active ACKR3 ligands. Notably, modification at the l-Pro position with a bulky hydrophobic side chain led to improved bioactivity toward ACKR3. |
| Databáze: | OpenAIRE |
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