Nuclear receptor-cofactor interaction

Evaluation of the Nuclear Receptor-Cofactor Interaction as a Drug Target... 

Small molecules constitute the ultimate goal in the search for compounds that can directly block the nuclear receptor-cofactor interaction. Such compounds would not only constitute a new pharmacological and cell biological tool to modulate nuclear receptor-regulated gene transcription, but are also envisaged to provide a new entry in nuclear receptor antagonism. 

The nuclear receptor-cofactor interaction, more specifically the nuclear receptor-coactivator interaction, has emerged as a drugable protein-protein interaction. Even though many aspects of its drugability are still unsolved, both the results obtained on the biological evaluation of its direct inhibition and the development of the first small-molecule inhibitors show the potential of targeting this interaction. 

The most important point of attention currently is the development of new and optimized CBIs with which the concept of inhibition of the nuclear receptor-cofactor interaction can be investigated in more detail and be possibly validated for... 

A field which is still far from being completely understood on a molecular level is the nuclear receptor-cofactor interaction. Luc Brunsveld, B. Vaz and S. Moddinghoff give an introduction to our current knowledge in this field and explain why these interactions might be attractive targets for more selective modulators. 

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