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Sammanfattning

The molecular mechanisms of oestrogens are more complicated than formerly assumed. Firstly, there are two variants of the oestrogen receptor, each with different influence on gene expression. Secondly, the two receptor subtypes are diferentially expressed in different tissue types and cell types. In addition, the ER-ligand-complex not only binds to classic oestrogen response elements (ERE) in the DNA but also directly to other sequences and indirectly to DNA through separate transcription factor complexes. Moreover, there are both corepressors and coactivators, which are recruited in varying degrees depending on ligand, DNA-sequence, and cell-type. These corepressors and coactivators modulate the function of the receptors. At the same time, the function of the receptor can be affected by phosphorylation and other modification, and finally oestrogens also possess non-genomic effects. They are able to initiate intracellular signal transduction pathways through interaction with membrane-bound or cytosolic proteins. All in all, a full insight into the molecular mechanisms of oestrogens, which will allow the design of both tissue-specific and cell-specific oestrogen modulators, are still far away.

MeSH