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1. (WO2018165575) WARHEAD-CONTAINING PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF BFL-1

Pub. No.:    WO/2018/165575    International Application No.:    PCT/US2018/021793
Publication Date: Fri Sep 14 01:59:59 CEST 2018 International Filing Date: Sat Mar 10 00:59:59 CET 2018
IPC: A61K 38/00
C07K 14/00
C07K 14/435
C07K 14/60
C07K 14/575
Applicants: AILERON THERAPEUTICS, INC.
Inventors: GUERLAVAIS, Vincent
Title: WARHEAD-CONTAINING PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF BFL-1
Abstract:
The disclosed peptidomimetic macrocycles modulate the activity of BFL-1 or a BCL-2 family protein. BFL-1, an anti-apoptotic BCL-2 family member, blocks p53-mediated apoptosis and has oncogenic transforming activity. Peptidomimetic macrocycles, pharmaceutical compositions, and methods disclosed herein can be used for the treatment of disease in which BFL-1 or a BCL-2 family protein is over-expressed, such as cancer. In particular, BFL-1-modulating or a BCL-2 family protein-modulating peptidomimetic macrocycles disclosed herein can be applied in the setting of resistance to BCL-2 family inhibitors, which is often engendered by BFL-1 or BCL-2 family protein over-expression or hyper-activation.