Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: A method is described to assay for protein interactions in living cells, e.g. by the introduction of two heterologous conjugates into the cell. The method uses the measurement of cellular distribution of a detectable component (e.g. a GFP-labeled˜fluorescent probe) to indicate the presence or absence of an interaction between that component and a second component of interest. The method uses the knowledge that certain components can be stimulated to redistribute within the cell to defined locations. Inducible redistribution systems make it possible to determine if specific interactions occur between components. Inducible systems are described where it is demonstrated that the redistribution stimuli are essentially “null”, in that they affect no other system in the cell during the assay period, other than the component whose redistribution can be induced.

Abstract: The present invention relates to various uses of complementing proteins protein fragments to discover chemical compounds or drugs interfering with protein translocation/redistribution and/or protein interactions. The invention takes advantage of the fact that many interacting proteins reside in separate and distinct locations prior to the activation of the signaling pathways in which they play their part. The invention also takes advantage of interaction domains (FRBP, FKBP12) that can be induced to interact. Specifically disclosed are GFP (EGFP, F64L mutated EYFP) complementation.

Abstract: A method is described to assay for protein interactions in living cells, e.g. by the introduction of two heterologous conjugates into the cell. The method uses the measurement of cellular distribution of a detectable component (e.g. a GFP-labelled fluorescent probe) to indicate the presence or absence of an interaction between that component and a second component of interest. The method uses the knowledge that certain components can be stimulated to redistribute within the cell to defined locations. Inducible redistribution systems make it possible to determine if specific interactions occur between components. Inducible systems are described where it is demonstrated that the redistribution stimuli are essentially “null”, in that they affect no other system in the cell during the assay period, other than the component whose redistribution can be induced.

Abstract: The present invention relates to a 3-part hybrid system for detection protein interactions in live mammalian cells and screening for compounds modulating such interactions. The method is fully compatible with HTS. The three hybrids are a first heterologous conjugate comprising an anchor protein that specifically binds to an internal structure within the cell conjugated to an interactor protein of type A, a second heterologous conjugate comprising an interactor protein of type B conjugated to the first protein of interest, a third heterologous conjugate comprising a second protein of interest conjugated to a detectable group. When applying a dimerizer compound, interactor proteins A and B bind to each other and if the two proteins of interest interact, the distribution of the detectable group will mimic the distribution of the anchor protein. However, if there is no interaction, the distribution of the detectable group will mimic the distribution of the second protein of interest.