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Biotinylated-spiperone ligands for quantum dot labeling of the dopamine D2 receptor in live cell cultures.

Abstract：

:We have synthesized 3 analogs of the dopamine D2 receptor (D2 DR) antagonist spiperone that can be conjugated to streptavidin-coated quantum dots via a pegylated biotin derivative. Using fluorescent imaging we demonstrate that substitution on the spiro position is tolerated, whilst the length and rigidity of a spacer arm attached to spiperone is important in controlling specific labeling as well as minimizing nonspecific labeling to cells and the surface of cell culture dishes. The ligand with the most rigid linker IDT772 (4) had the best binding profile and had high specific binding to D2 DR expressing HEK-293T cells with low nonspecific binding to plates and HEK-293T cells that lacked the D2 DR.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tomlinson ID,Kovtun O,Crescentini TM,Rosenthal SJ

doi

10.1016/j.bmcl.2019.02.024

subject

Has Abstract

pub_date

2019-04-15 00:00:00

pages

959-964

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30109-X

journal_volume

29

pub_type

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