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11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is essential for the local activation of glucocorticoid receptors (GR). Unlike unliganded cytoplasmic GR, 11β-HSD1 is an endoplasmic reticulum (ER)-membrane protein with lumenal orientation. Cortisone might gain direct access to 11β-HSD1 by free diffusion across membranes, indirectly via intracellular binding proteins or, alternatively, by insertion...
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