IAP-based biodegraders can convert necroptosis to apoptosis and eliminate cancer driving protein complexes
Xiuquan Ma1, François Vaillant1, Deepagan Gopal1
1The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, University of Melbourne, Parkville, VIC 3052, Australia.
Abstract:
Targeted protein degradation holds significant therapeutic potential. Intrabodies, such as nanobodies and monobodies, can degrade intracellular proteins via fusion to E3 ubiquitin ligases. Here, we developed multi-targeting biodegrader intrabodies using the RING domain of inhibitor of apoptosis (IAP) proteins, or the IAP-binding motif from Smac/DIABLO. When fused to monobodies recognizing the necroptosis effector mixed lineage kinase domain-like pseudokinase (MLKL), IAP-based intrabodies degraded both MLKL and IAPs, blocking necroptosis and sensitizing cells to apoptosis. The potent degradative ability of the IAP RING was demonstrated via fusion to distinct intrabodies, with those targeting RAS enabling IAP and RAS proto-oncogenes to be concurrently eliminated. Quantitative proteomics of select IAP-based intrabodies revealed additional degradation of the BAF chromatin-remodelling complex, uncovering IAP and BAF co-dependencies in cancer. This work establishes IAP-based intrabodies as a modular class of protein biodegraders, whose multi-targeting capacity can enable the redirection of damaging necrotic cell death toward apoptosis, and the eradication of cancer-drivers.
Related Concept Videos
Autophagic Cell Death
Autophagy and Apoptosis
Autophagy can activate apoptosis. In normal conditions, the autophagy activating protein Beclin-1 and...
The Intrinsic Apoptotic Pathway
Phagocytosis of Apoptotic Cells
Normal cells contain receptors that prevent them from being recognized...
Necrosis
Morphological Manifestations of Necrosis
Necrotic cells show different types of morphological appearance depending on the type of tissue and infection. In coagulative necrosis, cells become...
Overview of Cell Death
Cell death was observed in the early 19th century, but there was no experimental evidence to prove it. In 1842, Carl Vogt first discovered cell death in a metamorphic toad; however, it was not termed ‘cell death.’ Scientists discovered different cell death pathways only in the...
The Extrinsic Apoptotic Pathway


