Design and Synthesis of Fluorescence-Labeled TAK779 Analogs as Chemical Probes

Design and Synthesis of Fluorescence-Labeled TAK779 Analogs as Chemical Probes

<i>N,N</i>-Dimethyl <i>N</i>-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5<i>H</i>-benzocyclohepten-8-yl]carbonyl]amino]benzyl]tetra-hydro-2<i>H</i>-pyran-4-aminium chloride (TAK779) has a potent binding affinity for the chemokine receptor CCR5 and low cytoto...

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Bibliographic Details
Main Authors: Hiroyuki Konno, Takuya Saito, Taichi Aota, Daiki Takanuma, Mizuho Okuyama, Chikako Yokoyama
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Molecules
Subjects:
TAK779
molecular probe
cell penetration
Online Access:https://www.mdpi.com/1420-3049/30/12/2655
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Summary:<i>N,N</i>-Dimethyl <i>N</i>-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5<i>H</i>-benzocyclohepten-8-yl]carbonyl]amino]benzyl]tetra-hydro-2<i>H</i>-pyran-4-aminium chloride (TAK779) has a potent binding affinity for the chemokine receptor CCR5 and low cytotoxicity; however, their interaction remains unknown. We designed and synthesized four fluorescence-labeled TAK779 analogs as chemical probes. Although the binding properties of the fluorescence-labeled TAK779 analogs for CCR5 could not be determined, it was found that they penetrate the cell membranes and localize to the microtubes of HeLa cells.
ISSN:1420-3049

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