Structural and functional analysis of Taspase1

Taspase1 is an endoprotease that hydrolyzes the human MLL and the oncofusion protein AF4-MLL at distinct cleavage sites (CS1 and CS2). It has been demonstrated that both protein complexes require Taspase1 for protein stability and proper function. In terms of t(4;11) leukemia, Taspase1 represents a conditional oncoprotein because Taspase1 cleaves AF4-MLL to form a high molecular weight complex that causes proB ALL. Therefore, we are aiming to identify potential inhibitors against Taspase1. Unfortunately, any efforts to target the enyzmatic center of Taspase1 have failed so far. For the purpose of our studies, we…