公开(公告)号：US20240246941A1

公开(公告)日：2024-07-25

申请号：US18015657

申请日：2021-07-15

Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, INC.

Inventor： Ryan POTTS ,  Taosheng CHEN ,  Zoran RANKOVIC ,  Jaeki MIN ,  Wenwei LIN ,  Seung Wook YANG ,  Anand MAYASUNDARI

IPC: C07D405/12 ,  A61K31/4706 ,  A61K31/4709 ,  A61K45/06 ,  A61P35/00 ,  C07D215/46 ,  C07D401/12 ,  C07K7/08

CPC classification number: C07D405/12 ,  A61K31/4706 ,  A61K31/4709 ,  A61K45/06 ,  A61P35/00 ,  C07D215/46 ,  C07D401/12 ,  C07K7/08

Abstract: Testis-restricted melanoma antigen (MAGE) proteins are frequently hijacked in cancer and play a critical role in tumorigenesis. These proteins assemble with E3 ubiquitin ligases and function as substrate adaptors that direct the ubiquitination of novel targets, including key tumor suppressors. However, the development of MAGE-directed therapeutics heretofore has been extremely limited. In one aspect, the disclosure relates to compounds and peptides useful as inhibitors of MAGE-All: substrate interaction, methods of making same, pharmaceutical compositions comprising same, and methods of treating a disorder associated with a MAGE-All dysfunction. e.g., a cancer, using same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.