# RECEPTOR MEDIATED RADIATION ONCOLOGY

> **NIH NIH R01** · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · 1991 · $208,920

## Abstract

The overall objective of the proposed research is to develop new
strategies in radiation oncology using the Auger effect of iodine-125
and the alpha emissions of astatine-211.  We will also synthesize and
evaluate the cytotoxicity of radiolabeled steroids and peptide hormones.
We will expand our understanding of receptor-mediated cytotoxicity using
iodinated steroid hormones and their analogues.

We will apply the strategies developed for breast cancer to other
steroid receptor containing tumors (viz., endometrium and prostate).
Both approaches offer the potential of specifically localizing lethal
amounts of ionizing radiation within target tumors while sparing the
surrounding normal tissue.

We will synthesize position specific, carrier-free 125-I-labeled
estrogens and progestins with high receptor affinity, prolonged nuclear
retention time and low non-specific binding.  The goals can be
accomplished using flourine substituted estrogen, 11b-methoxy
substitutions and mesylate/chloromethyl derivatives.  We will synthesize
several progesterones including fluorinated derivatives, iodo-
megesterol, an agent with enhanced PgR affinity, and iodomibolerone
which binds to both progesterone and androgen receptors.

We will synthesize 211-At-labeled steroids and peptide hormones (viz.,
prolactin and oxytocin) which, on the basis of 125-I studies, show high
receptor affinity for breast cancer cells.  We will also determine the
cytotoxicity of these compounds in breast cancer cell lines.

We will study the in vivo distribution and therapeutic activity of 125-I
and 211-At labeled steroid and peptide ligands in experimental tumor
models - MCF-7 cells in athymic mice, DMBA mammary tumors, LNCaP
prostatic carcinoma and MTW9 mammary adenocarcinoma.

This proposal aims to answer general quantitative questions about the
potential use of Auger and alpha emitters for radiation therapy.  The
research has significance at two levels - in the field of oncology, the
emphasis is on the possibility of using the radiotoxicity of Auger and
alpha emitters for cancer treatment; in the field of cellular and
molecular radiation biology, the emphasis is on the mechanism of action
of alpha particles and the Auger effect.

## Key facts

- **NIH application ID:** 3175345
- **Project number:** 5R01CA037553-06
- **Recipient organization:** UNIVERSITY OF PITTSBURGH AT PITTSBURGH
- **SAM.gov UEI:** MKAGLD59JRL1
- **Principal Investigator:** WILLIAM DAVID BLOOMER
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1991
- **Award amount:** $208,920
- **Award type:** 5
- **Project period:** 1984-04-01 → 1992-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3175345

## Citation

> US National Institutes of Health, RePORTER application 3175345, RECEPTOR MEDIATED RADIATION ONCOLOGY (5R01CA037553-06). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3175345. Licensed CC0.

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