Published in Molecular endocrinology (Baltimore, Md.)
The vitamin D receptor (VDR) mediates the endocrine actions of 1,25-dihydroxyvitamin D(3) [1,25(OH)(2)D(3)] and autoregulates the expression of its own gene in target cells. In studies herein, we used chromatin immunoprecipitation-chip analyses to examine further the activities of 1,25(OH)(2)D(3) and to assess the consequences of VDR/retinoid X rec...
Published in Molecular endocrinology (Baltimore, Md.)
Inherited mutations of the breast cancer susceptibility gene BRCA1 confer a high risk for breast cancer development. The (300)RXKK and (266)KXK motifs have been identified previously as sites for acetylation of the estrogen receptor-alpha (ER-alpha), and (302)K was also found to be a site for BRCA1-mediated mono-ubiquitination of ER-alpha in vitro....
Published in Molecular endocrinology (Baltimore, Md.)
Somatostatin analogs that activate the somatostatin subtype 2A (sst2A) receptor are used to treat neuroendocrine cancers because they inhibit tumor secretion and growth. Recently, new analogs capable of activating multiple somatostatin receptor subtypes have been developed to increase tumor responsiveness. We tested two such multi-somatostatin anal...
Published in Molecular endocrinology (Baltimore, Md.)
Selective estrogen receptor modulators (SERMs), such as tamoxifen (TAM), have been used extensively for the treatment and prevention of breast cancer and other pathologies associated with aberrant estrogen receptor (ER) signaling. These compounds exhibit cell-selective agonist/antagonist activities as a consequence of their ability to induce differ...
Published in Molecular endocrinology (Baltimore, Md.)
Vascular endothelial growth factor (VEGF) and endometrial angiogenesis play a critical role in successful embryonic implantation. Despite many studies of the effects of estrogen and progesterone on VEGF expression, its focal regulation at the site of implantation is unknown. Retinoic acid (RA) has been reported to regulate VEGF in a variety of cell...
Published in Molecular endocrinology (Baltimore, Md.)
Estrogen receptors ERalpha and ERbeta, members of the nuclear receptor superfamily, exert profound effects on the gene expression and biological response programs of their target cells. Herein, we explore the dynamic interplay between these two receptors in their selection of chromatin binding sites when present separately or together in MCF-7 brea...
Published in Molecular endocrinology (Baltimore, Md.)
An intractable problem impeding breast cancer treatment by the most frequently prescribed endocrine therapy tamoxifen is the inevitable development of resistance, and the molecular mechanisms underlying this loss of responsiveness by breast cancers have been under intense investigation but are not yet fully elucidated. Our recent reports demonstrat...
Published in Molecular endocrinology (Baltimore, Md.)
Rb/E2F is dysregulated in murine and human pituitary tumors. Pituitary tumor transforming gene (PTTG1), a securin protein, is required for pituitary tumorigenesis, and PTTG1 deletion attenuates pituitary tumor development in Rb(+/-) mice. E2F1 and PTTG1 were concordantly overexpressed in 29 of 46 Rb(+/-) murine pituitary tissues and also in 45 of 8...
Published in Molecular endocrinology (Baltimore, Md.)
Indole-3-carbinol and its diindole condensation product 3-3'-diindolylmethane are dietary phytochemicals that have striking anticarcinogenic properties in human cancer cells. Molecular, cellular, physiological, and clinical studies have documented that both indole-3-carbinol and 3-3'-diindolylmethane have potent endocrine modulating activities thro...
Published in Molecular endocrinology (Baltimore, Md.)
The role of phospholipase D (PLD) in the regulation of the traffic of the PTH type 1 receptor (PTH1R) was studied in Chinese hamster ovary cells stably transfected with a human PTH1R (CHO-R3) and in rat osteosarcoma 17/2.8 (ROS) cells. PTH(1-34) increased total PLD activity by 3-fold in CHO-R3 cells and by 2-fold in ROS cells. Overexpression of wil...
