Literature DB >> 20594864

Radiosynthesis and biological evaluation of a promising sigma(2)-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer.

Zhude Tu1, Jinbin Xu, Lynne A Jones, Shihong Li, Dexing Zeng, Mei-Ping Kung, Hank F Kung, Robert H Mach.   

Abstract

Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity sigma(2) receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [(18)F]3 and [(125)I]3, respectively. Studies of [(125)I]3 using murine 66 breast tumor membrane homogenates and evaluation of [(18)F]3 and [(125)I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging sigma(2) receptors in breast cancer. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20594864      PMCID： PMC2937058          DOI： 10.1016/j.apradiso.2010.06.004

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN： 0969-8043            Impact factor:   1.513


  19 in total

1.  A proposal for the classification of sigma binding sites.

Authors:  R Quirion; W D Bowen; Y Itzhak; J L Junien; J M Musacchio; R B Rothman; T P Su; S W Tam; D P Taylor
Journal:  Trends Pharmacol Sci       Date:  1992-03       Impact factor: 14.819

2.  Subcellular localization of sigma-2 receptors in breast cancer cells using two-photon and confocal microscopy.

Authors:  Chenbo Zeng; Suwanna Vangveravong; Jinbin Xu; Katherine C Chang; Richard S Hotchkiss; Kenneth T Wheeler; Duanwen Shen; Zhi-Ping Zhuang; Hank F Kung; Robert H Mach
Journal:  Cancer Res       Date:  2007-07-15       Impact factor: 12.701

3.  Overexpression of sigma receptors in nonneural human tumors.

Authors:  W T Bem; G E Thomas; J Y Mamone; S M Homan; B K Levy; F E Johnson; C J Coscia
Journal:  Cancer Res       Date:  1991-12-15       Impact factor: 12.701

4.  [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe.

Authors:  Jinbin Xu; Zhude Tu; Lynne A Jones; Suwanna Vangveravong; Kenneth T Wheeler; Robert H Mach
Journal:  Eur J Pharmacol       Date:  2005-11-10       Impact factor: 4.432

5.  Sigma 2 receptors as potential biomarkers of proliferation in breast cancer.

Authors:  R H Mach; C R Smith; I al-Nabulsi; B R Whirrett; S R Childers; K T Wheeler
Journal:  Cancer Res       Date:  1997-01-01       Impact factor: 12.701

6.  Purification, molecular cloning, and expression of the mammalian sigma1-binding site.

Authors:  M Hanner; F F Moebius; A Flandorfer; H G Knaus; J Striessnig; E Kempner; H Glossmann
Journal:  Proc Natl Acad Sci U S A       Date:  1996-07-23       Impact factor: 11.205

7.  Carbon-11 labeled sigma2 receptor ligands for imaging breast cancer.

Authors:  Zhude Tu; Carmen S Dence; Datta E Ponde; Lynne Jones; Kenneth T Wheeler; Michael J Welch; Robert H Mach
Journal:  Nucl Med Biol       Date:  2005-07       Impact factor: 2.408

8.  Characterization of a novel iodinated sigma-2 receptor ligand as a cell proliferation marker.

Authors:  Catherine Hou; Zhude Tu; Robert Mach; Hank F Kung; Mei-Ping Kung
Journal:  Nucl Med Biol       Date:  2006-02       Impact factor: 2.408

9.  Rat liver and kidney contain high densities of sigma 1 and sigma 2 receptors: characterization by ligand binding and photoaffinity labeling.

Authors:  S B Hellewell; A Bruce; G Feinstein; J Orringer; W Williams; W D Bowen
Journal:  Eur J Pharmacol       Date:  1994-06-15       Impact factor: 4.432

10.  Sigma-1 and sigma-2 receptors are expressed in a wide variety of human and rodent tumor cell lines.

Authors:  B J Vilner; C S John; W D Bowen
Journal:  Cancer Res       Date:  1995-01-15       Impact factor: 12.701
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  12 in total

1.  Design and Investigation of a [18F]-Labeled Benzamide Derivative as a High Affinity Dual Sigma Receptor Subtype Radioligand for Prostate Tumor Imaging.

Authors:  Dongzhi Yang; Anthony Comeau; Wayne D Bowen; Robert H Mach; Brian D Ross; Hao Hong; Marcian E Van Dort
Journal:  Mol Pharm       Date:  2017-02-14       Impact factor: 4.939

2.  Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for binding σ1 and σ2 receptors.

Authors:  Kuo-Hsien Fan; John R Lever; Susan Z Lever
Journal:  Bioorg Med Chem       Date:  2011-02-12       Impact factor: 3.641

Review 3.  Current molecular imaging positron emitting radiotracers in oncology.

Authors:  Aizhi Zhu; Hyunsuk Shim
Journal:  Nucl Med Mol Imaging       Date:  2011-02-01

Review 4.  The σ2 receptor: a novel protein for the imaging and treatment of cancer.

Authors:  Robert H Mach; Chenbo Zeng; William G Hawkins
Journal:  J Med Chem       Date:  2013-06-18       Impact factor: 7.446

5.  Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands.

Authors:  Suping Bai; Shihong Li; Jinbin Xu; Xin Peng; Kiran Sai; Wenhua Chu; Zhude Tu; Chenbo Zeng; Robert H Mach
Journal:  J Med Chem       Date:  2014-05-12       Impact factor: 7.446

6.  Breast Cancer 18F-ISO-1 Uptake as a Marker of Proliferation Status.

Authors:  Elizabeth S McDonald; Robert K Doot; Anthony J Young; Erin K Schubert; Julia Tchou; Daniel A Pryma; Michael D Farwell; Anupma Nayak; Amy Ziober; Michael D Feldman; Angela DeMichele; Amy S Clark; Payal D Shah; Hsiaoju Lee; Sean D Carlin; Robert H Mach; David A Mankoff
Journal:  J Nucl Med       Date:  2019-12-13       Impact factor: 10.057

7.  Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2.

Authors:  Zonghua Luo; Qianwa Liang; Hui Liu; Joshi Sumit; Hao Jiang; Robyn S Klein; Zhude Tu
Journal:  Nucl Med Biol       Date:  2020-07-27       Impact factor: 2.408

8.  Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site.

Authors:  Jinbin Xu; Chenbo Zeng; Wenhua Chu; Fenghui Pan; Justin M Rothfuss; Fanjie Zhang; Zhude Tu; Dong Zhou; Dexing Zeng; Suwanna Vangveravong; Fabian Johnston; Dirk Spitzer; Katherine C Chang; Richard S Hotchkiss; William G Hawkins; Kenneth T Wheeler; Robert H Mach
Journal:  Nat Commun       Date:  2011-07-05       Impact factor: 14.919

9.  The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine.

Authors:  John R Hornick; Jinbin Xu; Suwanna Vangveravong; Zhude Tu; Jonathan B Mitchem; Dirk Spitzer; Peter Goedegebuure; Robert H Mach; William G Hawkins
Journal:  Mol Cancer       Date:  2010-11-22       Impact factor: 27.401

10.  Synthesis and Characterization of a Specific Iodine-125-Labeled TRPC5 Radioligand.

Authors:  Yanbo Yu; Qianwa Liang; Lixia Du; Hao Jiang; Jiwei Gu; Hongzhen Hu; Zhude Tu
Journal:  ChemMedChem       Date:  2020-09-02       Impact factor: 3.540
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