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

## TL;DR

Researchers created fluorescent versions of a drug called TAK779 to study its behavior in cells, finding it enters cells and localizes in microtubes.

## Contribution

The novel contribution is the design and synthesis of fluorescence-labeled TAK779 analogs for cellular localization studies.

## Key findings

- Fluorescence-labeled TAK779 analogs penetrate cell membranes.
- The analogs localize to microtubes in HeLa cells.
- Binding properties for CCR5 could not be determined.

## Abstract

N,N-Dimethyl N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl]carbonyl]amino]benzyl]tetra-hydro-2H-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.