University of Illinois

Memorial Sloan Kettering Cancer Center

Stevens Institute of Technology

Sarat Chandarlapaty

John A Katzenellenbogen

Weiyi Toy

Abhishek Sharma

Shengjia Lin

Lucia Wang

A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized. 

Antiestrogen compounds

Growing community of inventors

New York, NY, United States of America

Sarat Chandarlapaty