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Vol. 289, Issue 1, 251-260, April 1999

Molecular and Ligand-Binding Characterization of the sigma -Receptor in the Jurkat Human T Lymphocyte Cell Line1

Malliga E. Ganapathy, Puttur D. Prasad, Wei Huang, Pankaj Seth, Frederick H. Leibach and Vadivel Ganapathy

From the Departments of Medicine (M.E.G.), Biochemistry and Molecular Biology (W.H., P.S., F.H.L., V.G.), and Obstetrics and Gynecology (P.D.P.), Medical College of Georgia, Augusta, Georgia

The sigma  binding site present in the Jurkat human T lymphocyte cell line was investigated. Jurkat cell membranes were found to have a single saturable binding site for [3H]haloperidol, a sigma  ligand (dissociation constant, 3.9 ± 0.3 nM). The binding of [3H]haloperidol was inhibited by several sigma  ligands. Northern analysis and reverse transcription-polymerase chain reaction provided evidence for the expression of the recently cloned type 1 sigma -receptor (sigma -R1) in Jurkat cells. The sigma -R1 cDNA cloned from these cells was functional in heterologous expression systems. When expressed in mammalian cells, the cDNA-induced binding was saturable with dissociation constants of 1.9 ± 0.3 nM for [3H]haloperidol and 12 ± 2 nM for (+)-pentazocine. The binding of [3H]progesterone, a putative endogenous ligand to sigma -R1, to the Jurkat cell sigma -receptor could be directly demonstrated by using heterologously expressed sigma -R1 cDNA. The binding of [3H]progesterone was saturable, with a dissociation constant of 88 ± 7 nM. Progesterone and haloperidol interacted with the receptor competitively. Reverse transcription-polymerase chain reaction also produced evidence for the existence of an alternatively spliced sigma -R1 variant in Jurkat cells. This splice variant was found to be nonfunctional in ligand binding assays. This constitutes the first report on the molecular characterization of the sigma -receptor in immune cells.

0022-3565/99/2891-0251$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 1999 by The American Society for Pharmacology and Experimental Therapeutics


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