Novel Chemical Strategies for Labeling Small Molecule Ligands for Androgen, Progestin, and Peroxisome Proliferator-Activated Receptors for Imaging Prostate and Breast Cancer and the Heart [electronic resource].
- Published
- Washington, D.C. : United States. Dept. of Energy. Office of Energy Research, 2007.
Oak Ridge, Tenn. : Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy. - Physical Description
- 1,326 KB : digital, PDF file
- Additional Creators
- University of Illinois at Urbana-Champaign, United States. Department of Energy. Office of Energy Research, and United States. Department of Energy. Office of Scientific and Technical Information
Access Online
- Restrictions on Access
- Free-to-read Unrestricted online access
- Summary
- Summary of Progress The specific aims of this project can be summarized as follows: • Aim 1: Prepare and evaluate radiolabeled ligands for the peroxisome proliferator-activated receptor (PPAR), a new nuclear hormone receptor target for tumor imaging and hormone therapy. • Aim 2: Prepare steroids labeled with a cyclopentadienyl tricarbonyl technetium or rhenium unit. • Aim 3: Prepare and evaluate other organometallic systems of novel design as ligand mimics and halogenated ligands for nuclear hormone receptor-based tumor imaging. As is described in detail below, we made excellent progress on all three of these aims; the highlights of our progress are the following: • we have prepared the first fluorine-18 labeled analogs of ligands for the PPAR receptor and used these in tissue distribution studies in rats • we have developed three new methods for the synthesis of cyclopentadienyltricarbonyl rhenium and technetium (CpRe(CO)3 and CpTc(CO)3) systems and we have adapted these to the synthesis of steroids labeled with these metals, as well as ligands for other receptor systems • we have prepared a number of fluorine-18 labeled steroidal and non-steroidal androgens and measured their tissue distribution in rats • we have prepared iodine and bromine-labeled progestins with high progesterone receptor binding affinity • we have prepared inorganic metal tricarbonyl complexes and steroid receptor ligands in which the metal tricarbonyl unit is an integral part off the ligand core.
- Report Numbers
- E 1.99:doe/er/60401-3
doe/er/60401-3 - Subject(s)
- Other Subject(s)
- Affinity
- Androgens
- Fluorine 18.
- Hormones
- Iodine
- Mammary Glands
- Neoplasms
- Progesterone
- Prostate
- Rhenium
- Steroids
- Synthesis
- Targets
- Technetium
- Therapy
- Tissue Distribution
- Fluorine-18, Bromine-76, Androgen Receptor, Progesterone Receptor, Peroxisome Proliferator-Activated Receptor, Breast Cancer, Prostate Cancer, Positron Emission Tomography, Tumor Imaging
- Note
- Published through SciTech Connect.
04/19/2007.
"doe/er/60401-3"
Katzenellenbogen, John, A. - Type of Report and Period Covered Note
- Final; 02/01/1998 - 05/31/2006
- Funding Information
- FG02-86ER60401
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