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Bioorg Chem 2021 Mar 30;111:104878. Epub 2021 Mar 30.

Laboratory of Protein Biochemistry, Faculty of Biotechnology, University of Wrocław, Joliot-Curie 14a, 50-383 Wrocław, Poland. Electronic address:

The hypercalcemic effects of the hormone 1α,25-dihydroxyvitamin D (calcitriol) and most of known vitamin D metabolites and analogs call for the development of non secosteroidal vitamin D receptor (VDR) ligands as new selective and noncalcemic agonists for treatment of hyperproliferative diseases. We report on the in silico design and stereoselective synthesis of six lithocholic acid derivatives as well as on the calcemic activity of a potent LCA derivative and its crystallographic structure in complex with zVDR LBD. The low calcemic activity of this compound in comparison with the native hormone makes it of potential therapeutic value. Read More

J Cardiovasc Pharmacol 2021 Apr 9. Epub 2021 Apr 9.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Alexandria University Alexandria, Egypt. Department of Pharmacology and Toxicology, Faculty of Medicine, Kuwait University, Kuwait.

Abstract: Inconsistent reports are available on the role of testosterone in end-organ damage caused by endotoxemia. Here, pharmacologic, surgical, and molecular studies were employed to assess the testosterone modulation of cardiovascular, autonomic, and peripheral and central inflammatory derangements caused by endotoxemia. Studies were performed in conscious male rats pre-instrumented with femoral indwelling catheters for measurement of blood pressure and subjected to castration or pharmacologic interventions that interrupt the biosynthetic cascade of testosterone. Read More

Eur J Endocrinol 2021 Apr 1. Epub 2021 Apr 1.

M Kluge, Department of Psychiatry and Psychotherapy, University of Leipzig Faculty of Medicine, Leipzig, Germany.

Objective: Ghrelin is an orexigenic peptide hormone involved in the regulation of energy homeostasis, food intake and glucose metabolism. Serum levels increase anticipating a meal and fall afterwards. Underlying genetic mechanisms of the ghrelin secretion are unknown. Read More

J Mol Endocrinol 2021 Apr 1. Epub 2021 Apr 1.

K Miura, Department of Aging and Longevity Research, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan.

Naked mole-rats (Heterocephalus glaber) inhabit subterranean burrows in savannas and are thus unable to access free water. To identify their mechanism of osmoregulation in xeric environments, we molecularly cloned and analyzed the mineralocorticoid receptor (MR) gene, required for hormone-dependent regulation of genes contributing to body fluid homeostasis. Most vertebrates harbor a single MR homolog. Read More

Eur J Endocrinol 2021 Apr 1. Epub 2021 Apr 1.

K Ho, Diabetes, Garvan Institute of Medical Research, Darlinghurst, Australia.

There is a strong biological link between the GH and gonadal systems in growth, development and metabolism; however regulatory interactions are poorly understood. Advances in estrogen biology and endocrine physiology have provided insights into mechanistic links between the two systems. Estrogens are synthesised from androgens by aromatase which is widely distributed in extragonadal tissues. Read More