Publications by authors named "Aleksandar Jamborcic"
Article Synopsis
- Targeted protein degradation (TPD) using the ubiquitin proteasome system (UPS) is emerging as a promising approach for drug discovery, focusing on eliminating harmful proteins.
- The study identifies and optimizes a small molecule, PLX-3618, which selectively degrades the BRD4 protein, demonstrating strong antitumor effects in lab tests and animal models.
- The research uncovers DCAF11 as the crucial E3 ligase that activates this degradation process, establishing a specific interaction among BRD4, PLX-3618, and DCAF11.
Targeted protein degradation (TPD) using the ubiquitin proteasome system (UPS) is a rapidly growing drug discovery modality to eliminate pathogenic proteins. Strategies for TPD have focused on heterobifunctional degraders that often suffer from poor drug-like properties, and molecular glues that rely on serendipitous discovery. Monovalent "direct" degraders represent an alternative approach, in which small molecules bind to a target protein and induce degradation of that protein through the recruitment of an E3 ligase complex.
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