Targeting Cell Surface Receptors with Ligand-Conjugated Nanocrystals

Citations Over TimeTop 1% of 2002 papers

Abstract

To explore the potential for use of ligand-conjugated nanocrystals to target cell surface receptors, ion channels, and transporters, we explored the ability of serotonin-labeled CdSe nanocrystals (SNACs) to interact with antidepressant-sensitive, human and Drosophila serotonin transporters (hSERT, dSERT) expressed in HeLa and HEK-293 cells. Unlike unconjugated nanocrystals, SNACs were found to dose-dependently inhibit transport of radiolabeled serotonin by hSERT and dSERT, with an estimated half-maximal activity (EC(50)) of 33 (dSERT) and 99 microM (hSERT). When serotonin was conjugated to the nanocrystal through a linker arm (LSNACs), the EC(50) for hSERT was determined to be 115 microM. Electrophysiology measurements indicated that LSNACs did not elicit currents from the serotonin-3 (5HT(3)) receptor but did produce currents when exposed to the transporter, which are similar to those elicited by antagonists. Moreover, fluorescent LSNACs were found to label SERT-transfected cells but did not label either nontransfected cells or transfected cells coincubated with the high-affinity SERT antagonist paroxetine. These findings support further consideration of ligand-conjugated nanocrystals as versatile probes of membrane proteins in living cells.

Related Papers

• → Simultaneous control of nanocrystal size and nanocrystal-nanocrystal separation in CdS nanocrystal assembly(2005)55 cited
• → Manipulating the Charging Energy of Nanocrystal Arrays(2005)37 cited
• → The first soluble conjugated poly(2,6-anthrylene): synthesis and properties(2007)28 cited
• → Modeling of Nanocrystal Storage Cells(2009)
• Hierarchical mechanical behavior of cobalt supracrystals related to nanocrystallinity(2015)