Bioorganic & Medicinal Chemistry Letters 2011-10-01

Synthesis of a quinazoline derivative: a new α₁-adrenoceptor ligand for conjugation to quantum dots to study α₁-adrenoceptors in living cells.

Guoheng Zhou, Lei Wang, Yudao Ma, Liping Wang, Youyi Zhang, Wei Jiang

Index: Bioorg. Med. Chem. Lett. 21(19) , 5905-9, (2011)

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Abstract

Quantum dots (QDs) that are conjugated to small molecule derivatives of drugs and endogenous ligands may be useful tools to study the distribution and dynamic of membrane bound receptors, ion channels and transporters in live cells. In order to use these tools, it is necessary to functionalize QDs with bioactive ligands. In this paper, we successfully synthesized a ligand of α(1)-adrenoceptor that could be conjugated to QDs. In addition, the conjugation of the ligands to QDs and their biological activity were evaluated through binding assay with 30 nM QD conjugates in living human embryonic kidney 293 cells.Copyright © 2011 Elsevier Ltd. All rights reserved.