SERM-receptor complexes

Thus, for effective gene transcription, programmed and targeted by the shape and phosphorylation status of ER and coactivators, a dynamic and cyclic process of transcription complex assembly [255] and destruction of transcription complexes by the proteasome is required. Estrogen- and SERM-receptor complexes have differing accumulation patterns in the target cell nucleus [151, 256] primarily because the relative rates of destruction of the complexes are different [251]. 

The availability of coactivators in that cell line that recognize the receptor-SERM complex that, at the same time, is subject to a regulation of its expression, to competition, as they may be in the process of being recruited by other receptors, etc. 

Vessieres A, Top S, Beck W, Hillard EA, Jaouen G (2006) Metal complex SERMs (Selective Estrogen Receptor Modulators). The influence of different metal units on breast cancer cell antiproliferative effects. Dalton Trans 4 529-541... 

SERMs). Tliey ciinnoi be classified simply as agoni.sts or antagonists. Rather they can be considered variable agonists ami antagonists. Tlicir selectivity is very complex because it depends on the organ in which the receptor is located. 

This approach was followed concurrendy with that of steroids as part of platinum coordination complexes for which the principal target was found to be DNA. Despite many structural modifications, the results were not spectacular [104-106]. Very often these Pt hybrids or their associated SERMs provided no synergy [107], as far as new, useftil properties were concerned. On the other hand, with covalent organometallic complexes, a number of pioneering results made it possible to study their recognition for specific nuclear receptors, and to develop novel affinity markers or suicide substrates. These preferentially targeted key proteins in specific biological functions to the detriment of DNA. 

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