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
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.
- Research Organization:
- University of Illinois, Urbana-Champaign
- Sponsoring Organization:
- USDOE - Office of Energy Research (ER)
- DOE Contract Number:
- FG02-86ER60401
- OSTI ID:
- 902426
- Report Number(s):
- DOE/ER/60401-3; TRN: US0806202
- Country of Publication:
- United States
- Language:
- English
Similar Records
Radiolabeled androgens and progestins as imaging agents for tumors of the prostate and breast. Technical progress report, February 1, 1992--January 31, 1993
(Fluorine-18 labeled androgens and progestins: Imaging agents for tumors of the prostate and breast)
Related Subjects
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