Eugene R. DeSombre

Learn 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)
Long-term administration of [D-Leu6, des-Gly-NH210, Pro-ethylamide9]-GnRH, an analog of gonadotropin releasing hormone, caused regression of neoplastic tissue in a rat bearing a spontaneous mammary adenocarcinoma and in rats in which tumors had been induced by treatment with dimethylbenzanthracene (DMBA). During two separate treatment periods with the(More)
This study compares the specific uptake and retention of the Z and E isomers of 17 alpha-iodovinyl-11 beta-methoxyestradiol (IVME2) in estrogen target tissues in immature female rats following intraperitoneal injection. Estrogen receptor binding studies in vitro showed that the Z-IVME2 had greater affinity than the E-IVME2, but our initial in vivo data,(More)
The topographical changes of the luminal surface of the endometrium of immature and ovariectomized rats treated with estrogen, antagonists to estrogen, and progesterone. and during various stages of the estrous cycle and in pregnancy were examined by scanning electron microscopy. Massive increases in numbers and length of endometrial cell microvilli were(More)
The estrogen antagonist C1628 maintains sustained hypertrophy of the uterine epithelium and the synthesis of many proteins including peroxidase. C1628 is a progestogen, inducing secretion of the protein by surface epithelial and glandular cells. C1628 is a connective tissue mitogen, inducing DNA synthesis in fibroblasts and the endothelium. C1628 and(More)
Data derived from a correlated morphological and biochemical study suggest the following: (a) estradiol-17beta, diethylstilbestrol, the estrogen antagonists nafoxidine (Upjohn 11,000), and Parke Davis C1628 induce synthesis of an endogenous peroxidase in the epithelium of target tissues like the vagina, the cervix, the uterus, and in the acinar cells of the(More)
SUMMARY The potent antiestrogen, Parke-Davis CI628, was evalu ated for its ability to effect regression of 7,12-dimethyl benz(a)anthracene-induced mammary tumors in the Sprague-Dawley rat. Chronic administration of this anties trogen resulted in regression of the majority of the tumors; about one-fourth of the tumors disappeared. The desired inhibition of(More)
A series of three 1,1-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)-ethylene derivatives was prepared and evaluated as potential estrogen receptor imaging agents. The compounds display high binding affinity compared to estradiol, with the 2-iodo and 2-bromo-derivatives expressing higher affinity than the parent 2-nonhalogenated derivative. Evaluation in immature(More)
As part of our program to develop novel ligands for the estrogen receptor, we synthesized the series of isomeric 17alpha-(trifluoromethyl)phenylvinyl estradiols using our solid-phase organic synthesis methodology. The compounds were evaluated for their relative binding affinity (RBA) using the ERalpha-LBD and in vivo potency using the immature rat(More)
  • 1