Ontology highlight
ABSTRACT:
SUBMITTER: Ramaswamy K
PROVIDER: S-EPMC5760651 | biostudies-literature | 2018 Jan
REPOSITORIES: biostudies-literature
Nature communications 20180109 1
Aberrant gene expression is a hallmark of acute leukemias. MYB-driven transcriptional coactivation with CREB-binding protein (CBP)/P300 is required for acute lymphoblastic and myeloid leukemias, including refractory MLL-rearranged leukemias. Using structure-guided molecular design, we developed a peptidomimetic inhibitor MYBMIM that interferes with the assembly of the molecular MYB:CBP/P300 complex and rapidly accumulates in the nuclei of AML cells. Treatment of AML cells with MYBMIM led to the ...[more]