Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists

• Published in: European journal of medicinal chemistry Vol. 51; pp. 184 - 192
• Main Authors: Wijtmans, Maikel, Maussang, David, Sirci, Francesco, Scholten, Danny J., Canals, Meritxell, Mujić-Delić, Azra, Chong, Milagros, Chatalic, Kristell L.S., Custers, Hans, Janssen, Elwin, de Graaf, Chris, Smit, Martine J., de Esch, Iwan J.P., Leurs, Rob
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 01.05.2012; Elsevier
• Subjects: 3D fingerprint; Agonist; Amides - chemistry; Biological and medical sciences; Chemistry Techniques, Synthetic; Chemistry, Medicinal; CXCR7; HEK293 Cells; Humans; Internalization; Life Sciences & Biomedicine; Ligand; Medical sciences; Miscellaneous; Models, Molecular; Molecular Conformation; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Quantitative Structure-Activity Relationship; Receptors, CXCR - agonists; Science & Technology; Styrene - chemical synthesis; Styrene - chemistry; Styrene - pharmacology; β-arrestin2; BRET; Agonist; RT; YFP; Ligand; EDCI; LDA; β-arrestin2; CXCR7; Cm; MIF; RLuc; CzH; FLAP; Internalization; HOBT; GPCR; NOESY; 3D fingerprint; HBSS; ELISA; ERK; MIGRATION; RDC1; CHEMOKINE RECEPTOR CXCR7; beta-arrestin2

The chemokine receptor CXCR7 is an atypical G protein-coupled receptor as it preferentially signals through the β-arrestin pathway rather than through G proteins. CXCR7 is thought to be of importance in cancer and the development of CXCR7-targeting ligands is of huge importance to further elucidate...