Published: 31 Dec 2025
Covalent BH3-Mimetics and PROTACs: Targeting BCL2 Family for Precision Apoptosis Induction
Volume 1
The BCL2 family of proteins serves as a central regulator of mitochondrial outer membrane permeabilization (MOMP) and intrinsic apoptosis, with anti-apoptotic members such as BCL2, BCL-XL, and MCL1 frequently overexpressed in many cancers to evade programmed cell death. Traditional BH3 mimetics, such as venetoclax and navitoclax, have revolutionized the treatment of hematologic malignancies by competitively inhibiting these pro-survival proteins. Yet, they face challenges, including acquired resistance, on-target toxicities, and limited..