Abstract: The invention provides compounds of formula (I), that are peptidase enhanced cytotoxics. The invention further provides pharmaceutical compositions comprising the compounds, and the use of the compounds or pharmaceutical compositions as a medicament, particularly for use in the treatment or prophylaxis of cancers such as multiple myeloma, osteosarcoma, breast cancer, lung cancer, ovarian cancer, leukaemia and lymphoma.

Abstract: The present invention is in the fields of biotechnology, protein purification and crystallization, x-ray diffraction analysis, three-dimensional computer molecular modelling and rational drug design. The invention is directed to the Liver X receptor and ligands for this receptor, and in particular to crystalline Liver X receptor beta (LXR?) and to methods of identifying ligands utilizing LXR?, as well as to compounds, compositions and methods for selecting, making, and using therapeutic or diagnostic agents having LXR? modulating or binding activity.