From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

The B cell lymphoma 2 (BCL-2) family of proteins has a key role in regulating apoptosis and is often dysregulated in cancer. This has led to the development of several inhibitors of pro-survival BCL-2 family proteins such as BCL-2, BCL-XL and MCL1, including the BCL-2 inhibitor venetoclax, which has recently gained regulatory approval. Here, Ashkenazi and colleagues discuss the latest progress in developing small-molecule inhibitors of pro-survival BCL-2 family proteins.