[EN] PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF MCL-1<br/>[FR] MACROCYCLES PEPTIDOMIMÉTIQUES EN TANT QUE MODULATEURS DE MCL-1
申请人:AILERON THERAPEUTICS INC
公开号:WO2017044633A1
公开(公告)日:2017-03-16
The disclosed peptidomimetic macrocycles such as Formula (Ic) that can modulate the activity of MCL-1. Myeloid cell leukemia 1 (MCL-1) is a protein that inhibits cell death. Peptidomimetic macrocycles, pharmaceutical compositions, and methods disclosed herein can be used for the treatment of disease in which MCL-1 is over-expressed, such as cancer. In particular, MCL- 1 -modulating peptidomimetic macrocycles disclosed herein can be applied in the setting of resistance to BCL-2 family inhibitors, which is often engendered by MCL-1 over-expression or hyperactivation.