Structural basis for the guanine nucleotide-binding activity of tissue transglutaminase and its regulation of transamidation activity

摘要

The present invention relates to methods of facilitating death of cancer cells in a subject by inhibiting tissue transglutaminase in the subject under conditions effective to facilitate death of cancer cells. Also disclosed are methods for identifying candidate compounds suitable for facilitating death of cancer cells in a subject by contacting tissue transglutaminase with a compound and identifying those compounds which bind to the tissue transglutaminase as candidate compounds suitable for facilitating death of cancer cells in a subject. The present invention also discloses methods of producing a tissue transglutaminase crystal suitable for X-ray diffraction as well as crystals produced by such methods. Also disclosed are compounds suitable for facilitating death of cancer cells in a subject as well as methods for designing such compounds.