Nat Med, 2012, 18(1):172-177

In vivo imaging of ligand receptor binding with Gaussia luciferase complementation

Studies of ligand-receptor binding and the development of receptor antagonists would benefit greatly from imaging techniques that translate directly from cell-based assays to living animals. We used Gaussia luciferase protein fragment complementation to quantify the binding of chemokine (C-X-C motif) ligand 12 (CXCL12) to chemokine (C-X-C motif) receptor 4 (CXCR4) and CXCR7. Studies established that small-molecule inhibitors of CXCR4 or CXCR7 specifically blocked CXCL12 binding in cell-based assays and revealed differences in kinetics of inhibiting chemokine binding to each receptor. Bioluminescence imaging showed CXCL12-CXCR7 binding in primary and metastatic tumors in a mouse model of breast cancer. We used this imaging technique to quantify drug-mediated inhibition of CXCL12-CXCR4 binding in living mice. We expect this imaging technology to advance research in areas such as ligand-receptor interactions and the development of new therapeutic agents in cell-based assays and small animals. © 2012 Nature America, Inc. All rights reserved.

Luker KE, Mihalko LA, Schmidt BT, Lewin SA, Ray P, Shcherbo D, Chudakov DM, Luker GD

IBCH: 4690
Ссылка на статью в журнале: http://www.nature.com/articles/nm.2590
Кол-во цитирований на 02.2024: 63
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