# STRUCTURE-FUNCTION RELATIONSHIP OF ANTIESTROGENS

> **NIH NIH R01** · UNIVERSITY OF WISCONSIN-MADISON · 1989 · $117,036

## Abstract

The non-steroidal antiestrogen, tamoxifen, is now accepted as a useful
therapeutic agent for the treatment of hormone-dependent breast cancer.
However, the pharmacology of antiestrogens has not been systemically
investigated and their molecular mechanism of action is unknown.  To
address these problems, we have developed an estrogen-sensitive pituitary
cell culture system.  The structure-activity relationship of antiestrogenic
ligands in the modulation of prolactin synthesis in rats and mice will be
studied following either in vivo treatment of animals or addition of
compounds to cultured rat and mouse pituitary cells.  We will investigate
whether the profound species differences in the action of antiestrogens
(rats vs mice) are due to altered ligand requirements or to differential
drug metabolism.  The basis for the opposite effects on prolactin synthesis
of estrogens and antiestrogens GH3 clonal rat pituitary tumor cells -
compared to normal pituitary cells - will be studied.  In selected
experiments, the relative abilities of antiestrogens to inhibit prolactin
synthesis and induce progesterone receptors will be compared.  Since
carcinogen-induced rat mammary cancer is known to be prolactin dependent,
our studies will provide precise data on an antitumor mechanism of
antiestrogens.

## Key facts

- **NIH application ID:** 3170578
- **Project number:** 5R01CA032713-08
- **Recipient organization:** UNIVERSITY OF WISCONSIN-MADISON
- **SAM.gov UEI:** LCLSJAGTNZQ7
- **Principal Investigator:** VIRGIL CRAIG JORDAN
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1989
- **Award amount:** $117,036
- **Award type:** 5
- **Project period:** 1982-08-01 → 1991-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3170578

## Citation

> US National Institutes of Health, RePORTER application 3170578, STRUCTURE-FUNCTION RELATIONSHIP OF ANTIESTROGENS (5R01CA032713-08). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3170578. Licensed CC0.

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