Eugene R Desombre

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The steroid hormone receptors are characterized by binding to relatively rigid, inflexible endogenous steroid ligands. Other members of the nuclear receptor superfamily bind to conformationally flexible lipids and show a corresponding degree of elasticity in the ligand-binding pocket. Here, we report the X-ray crystal structure of the oestrogen receptor(More)
The therapeutic potential for delivering a cytotoxic dose of radiation (using the decay of Auger-electron emitters) to the cell nucleus of cancer cells that express estrogen receptors (ERs) by radiolabeled estrogen was investigated in the ER-expressing human breast cancer cell line, MCF-7. The radiolabeled estrogen/ER complex irradiates the cell nucleus by(More)
During the past ten years much information has been accumulated concerning the interaction of tritiated estrogens with hormone-dependent tissues. Their striking affinity for estradiol, both in vivol-5 and in vitro,6-9 first suggested that such target tissues as uterus, vagina, and anterior pituitary possess unique components called "estrogen receptors."(More)
The interaction of estradiol with uterine cells involves the association of the hormone with an extranuclear receptor protein, followed by temperature dependent translocation of the resulting complex to the nucleus. During this process, the steroid binding unit of the protein undergoes an alteration, called "receptor transformation," that can be recognized(More)
The microTICAS image analysis system, originally designed for karyometry using Papanicolaou-stained or Feulgen-stained smears and tissue sections, has been adapted to assess tissue sections stained by immunohistochemical techniques. This system was used to quantitate growth fractions and the estrogen receptor (ER) content of breast carcinomas stained by(More)
Estrogen receptors alpha (ERalpha) and beta (ERbeta) have distinct functions and differential expression in certain tissues. These differences have stimulated the search for subtype-selective ligands. Therapeutically, such ligands offer the potential to target specific tissues or pathways regulated by one receptor subtype without affecting the other. As(More)
Transplanted mammary tumors growing in the inbred GR/AFib mouse were assayed for peroxidase activity and ability to concentrate injected 125I. Both tumor peroxidase activity and iodide uptake were about ten times greater in the hormone-resonsive (HR) tumors than in the hormone-independent tumors. However, although peroxidases are known for their ability to(More)
An estrogen receptor immunocytochemical assay which uses monoclonal antibodies to the estrogen receptor protein [Nature (Lond.), 307: 745-747, 1984] was applied to several human tissues, including human breast tumors, and the results were compared to those of steroid-binding assays performed on cytosol extracts of the same tissues. Specific immunoperoxidase(More)
Estrogen and prolactin receptor concentrations were measured in 24 carcinogen-induced rat mammary tumors and correlated with the tumor response to host ovariectomy or hypophysectomy. It was found that essentially all of the tumors contained some specific estrogen receptor, and all but three contained prolactin receptor. The values for each receptor(More)