Search results for " CYP450"
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Recent advances in computational design of potent aromatase inhibitors: open-eye on endocrine-resistant breast cancers.
2019
Introduction: The vast majority of breast cancers (BC) are estrogen receptor positive (ER+). The most effective treatments to fight this BC type rely on estrogen deprivation therapy, by inhibiting the aromatase enzyme, which performs estrogen biosynthesis, or on blocking the estrogens signaling path via modulating/degrading the estrogen's specific nuclear receptor (estrogen receptor-?, ER?). While being effective at early disease stage, patients treated with aromatase inhibitors (AIs) may acquire resistance and often relapse after prolonged therapies. Areas covered: In this compendium, after an overview of the historical development of the AIs currently in clinical use, and of the computati…
The immunological implications of the new Vitamin D metabolism
2018
Vitamin D is actually a neurohormone whose pleiotropic activities encompass regulation of calcium-phosphate metabolism, cell proliferation and immunomodulation. Starting from a cutaneous compound, 2 hydroxylation steps are required to produce the active form of vitamin D3, named calcitriol [1, 25-(OH)2-cholecalciferol]. The second hydroxylation step may occur at different tis- sues and cell types, including kidney, lung, prostate, brain, immune cells and placenta. Based on the advancing knowledge of Cytochrome P450 functions, a new conception of Vitamin D metabolism emerged. It implies that, depending on the site where the second hydroxylation step occurs, the active hormone can act as a ca…