Grafting a chromophore on AMD070 analogues for CXCR4 bioimaging: Chemical synthesis and in vitro assessment of the inhibition properties of the CXCR4 receptor

被引:0
作者
Roy, Marie M. Le [1 ]
Metivier, Cassandra
Le Saec, Patricia
Bouhsine, Hela [2 ]
Cherel, Michel [2 ]
Faivre-Chauvet, Alain [2 ]
Troadec, Thibault [1 ]
Tripier, Raphael [1 ]
机构
[1] Univ Brest, UMR CNRS CEMCA 6521, 6 Ave Victor Le Gorgeu, F-29200 Brest, France
[2] Univ Angers, Nantes Univ, Inserm UMR 1307, CNRS UMR 6075, CRCI 2,8 Quai Moncousu, F-44007 Nantes, France
关键词
CXCR4; AMD070; Fluorescence; HUMAN-IMMUNODEFICIENCY-VIRUS; SELECTIVE-INHIBITION; CHEMOKINE; BICYCLAM; ANTAGONISTS; EXPRESSION; POTENT; CORECEPTOR; PET/CT; ENTRY;
D O I
10.1016/j.bmcl.2024.130027
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Thank to their particular pharmacokinetics, the use of small organic molecules can be a very promising alternative to macromolecular targeting biomolecules (i.e. antibodies, peptides...) for specific imaging of tumours. Herein, the potential of two AMD070-like inhibitors as CXCR4-targeting units for specific imaging of cancer cells, and the influence of chromophore-grafting on their recognition properties was investigated.
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页数:5
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