T2857W is a kinase-inducible domain interacting (KIX) inhibitor designed from a peptide fragment corresponding to the transactivation domain (TAD) of the transcriptional activator, mixed-lineage leukemia protein (MLL). The KIX domain is an integral part of the general transcriptional coactivator CREB binding protein, and has been associated with leukemia, cancer, and various viral diseases. KIX is a small globular domain with two binding sites, the c-Myb site and MLL site, which bind the transcriptional activators c-Myb and MLL, respectively. T2857W is the mutant of the MLL TAD peptide identified as having the highest binding affinity for KIX from a series, with atwofold higher affinity for KIX than the wild-type MLL, and is effective in inhibiting the KIX-MLL interaction. T2857W also shows some selectivity for the MLL-KIX interaction over the c-Myb-KIX interaction.
