A novel functional translocator protein ligand for cancer imaging

被引:25
作者
Bai, Mingfeng
Rone, Malena B.
Papadopoulos, Vassilios
Bornhop, Darryl J. [1 ]
机构
[1] Vanderbilt Univ, Dept Chem, VU Stn B 351822, Stevenson Ctr 7300, Nashville, TN 37235 USA
[2] Georgetown Univ, Med Ctr, Dept Biochem & Mol & Cellular Biol, Washington, DC 20057 USA
关键词
D O I
10.1021/bc700251e
中图分类号
Q5 [生物化学];
学科分类号
071010 [生物化学与分子生物学]; 081704 [应用化学];
摘要
The translocator protein (TSPO) is an attractive target for tumor imaging due to its up-regulation in numerous cancer cell types. Here, we report a series of functional TSPO ligands, n-TSPOmbb732, which can be conjugated to a variety of signaling moieties and are widely applicable in TSPO-targeted molecular imaging. Two fluorescent dye-labeled 6-TSPOmbb732 displayed nanomolar binding affinities to TSPO and were successfully imaged in vitro.
引用
收藏
页码:2018 / 2023
页数:6
相关论文
共 15 条
[1]
A novel conjugable translocator protein ligand labeled with a fluorescence dye for in vitro imaging [J].
Bai, Mingfeng ;
Wyatt, Shelby K. ;
Han, Zeqiu ;
Papadopoulos, Vassilios ;
Bornhop, Darryl J. .
BIOCONJUGATE CHEMISTRY, 2007, 18 (04) :1118-1122
[2]
Binding characteristics of [3H]DAA1106, a novel and selective ligand for peripheral benzodiazepine receptors [J].
Chaki, S ;
Funakoshi, T ;
Yoshikawa, R ;
Okuyama, S ;
Okubo, T ;
Nakazato, A ;
Nagamine, M ;
Tomisawa, K .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1999, 371 (2-3) :197-204
[3]
Peripheral benzodiazepine receptor binding properties and effects on steroid synthesis of two new phenoxyphenyl-acetamide derivatives, DAA1097 and DAA1106 [J].
Culty, M ;
Silver, P ;
Nakazato, A ;
Gazouli, M ;
Li, H ;
Muramatsu, M ;
Okuyama, S ;
Papadopoulos, V .
DRUG DEVELOPMENT RESEARCH, 2001, 52 (03) :475-484
[4]
Decaudin D, 2002, CANCER RES, V62, P1388
[5]
GARNIER M, 1994, MOL PHARMACOL, V45, P201
[6]
CHEMISTRY, BINDING AFFINITIES, AND BEHAVIORAL PROPERTIES OF A NEW CLASS OF ANTINEOPHOBIC MITOCHONDRIAL DBI RECEPTOR COMPLEX (MDRC) LIGANDS [J].
KOZIKOWSKI, AP ;
MA, D ;
BREWER, J ;
SUN, S ;
COSTA, E ;
ROMEO, E ;
GUIDOTTI, A .
JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (20) :2908-2920
[7]
Novel peripheral benzodiazepine receptor ligand [11C]DAA1106 for PET:: An imaging tool for glial cells in the brain [J].
Maeda, J ;
Suhara, T ;
Zhang, MR ;
Okauchi, T ;
Yasuno, F ;
Ikoma, Y ;
Inaji, M ;
Nagai, Y ;
Takano, A ;
Obayashi, S ;
Suzuki, K .
SYNAPSE, 2004, 52 (04) :283-291
[8]
Mahmood U, 2003, MOL CANCER THER, V2, P489
[9]
A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening [J].
Manning, H. Charles ;
Smith, Sarah M. ;
Sexton, Michelle ;
Haviland, Sarah ;
Bai, Mingfeng ;
Cederquist, Kristin ;
Stella, Nephi ;
Bornhop, Darryl J. .
BIOCONJUGATE CHEMISTRY, 2006, 17 (03) :735-740
[10]
Facile, efficient conjugation of a trifunctional lanthanide chelate to a peripheral benzodiazepine receptor ligand [J].
Manning, HC ;
Goebel, T ;
Marx, JN ;
Bornhop, DJ .
ORGANIC LETTERS, 2002, 4 (07) :1075-1078