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Last-Step Pd-Mediated [C]CO Labeling of a Moxestrol-Conjugated o-Iodobenzyl Alcohol: From Model Experiments to in Vivo Positron Emission Tomography Studies.
Bioconjug Chem
November 2017
University of Bordeaux, CNRS, Institut des Sciences Moléculaires, UMR 5255 , 351 Cours de la Libération, 33405 Talence Cedex, France.
The fast, efficient, and functional group tolerant last-step radiolabeling of bioconjugates is crucial for positron emission tomography (PET) applications. In this context, o-iodobenzyl alcohol based structures were identified as ideal tags for an easy Pd-catalyzed carbonylation after bioconjugation, and a moxestrol-conjugated precursor was chosen as the model compound for the further studies. Despite scale and time constraints, conditions developed with [C]CO and [C]CO were easily transferred to the C isotope, and the desired radioactive product was obtained in amounts up to 740 MBq with radiochemical purities higher than 99%.
View Article and Find Full Text PDFSequence to structure approach of estrogen receptor alpha and ligand interactions.
Asian Pac J Cancer Prev
January 2016
Faculty of Veterinary Science, Mahidol University, Salaya, Nakhon-Pathom, Thailand E-mail :
Estrogen receptors (ERs) are steroid receptors located in the cytoplasm and on the nuclear membrane. The sequence similarities of human ERα, mouse ERα, rat ERα, dog ERα, and cat ERα are above 90%, but structures of ERα may different among species. Estrogen can be agonist and antagonist depending on its target organs.
View Article and Find Full Text PDFMolecular cloning, expression, and hormonal regulation of the chicken microsomal triglyceride transfer protein.
Gene
July 2013
Department of Medical Biochemistry, Medical University Vienna, Max F. Perutz Laboratories, A-1030 Vienna, Austria.
During an egg-laying cycle, oviparous animals transfer massive amounts of triglycerides, the major lipid component of very low density lipoprotein (VLDL), from the liver to the developing oocytes. A major stimulus for this process is the rise in estrogen associated with the onset of an egg-laying cycle. In mammals, the microsomal triglyceride transfer protein (MTP) is required for VLDL assembly and secretion.
View Article and Find Full Text PDFEstrogen modulates transactivations of SXR-mediated liver X receptor response element and CAR-mediated phenobarbital response element in HepG2 cells.
Exp Mol Med
November 2010
Department of Pharmaceutical Engineering, Jinju National University, Jinju 660-758, Korea.
The nuclear receptors, steroid and xenobiotic receptor (SXR) and constitutive androstane receptor (CAR) play important functions in mediating lipid and drug metabolism in the liver. The present study demonstrates modulatory actions of estrogen in transactivations of SXR-mediated liver X receptor response element (LXRE) and CAR-mediated phenobarbital response element (PBRU). When human estrogen receptor (hERα) and SXR were exogenously expressed, treatment with either rifampicin or corticosterone promoted significantly the SXR-mediated transactivation of LXRE reporter gene in HepG2.
View Article and Find Full Text PDFThe large number of reference data is proving the positive influence of exogenous hormones on the management of climacteric and dishormonal cardiomyopathies. However, the literary data concerning the influence of estrogens on the cardio-vascular system are quite controversial. For instance there is no certain opinion in the literature concerning influence of estrogens on the cardiovascular system of males, undergoing estrogen therapy due to prostate cancer.
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