eTPD is a distinct mode of targeted degradation of extracellular proteins.  eTPD utilizes bi-specific antibodies or small molecules that recruit membrane-bound or secreted target proteins to specific membrane-associated cycling receptors, transporting the cargo to lysosomes for degradation. Unlike PROTACs, eTPD  is not limited by the choice of E3 ligase ligands and can employ multiple degradation systems, offering better tissue selectivity.  Kinetics of degradation using eTPD modality may be slower compared to traditional PROTACs.

Some of the different eTPD strategies include:

  • Clearance Antibodies eTPD for Degradation of Soluble POI
  • Glycan-based Circulatory Receptor eTPD
  • eTPD Targeting Membrane Proteins Based on Transmembrane E3 Ligase
  • eTPD Targeting Membrane Proteins Based on Cytokines
  • Integrin-based eTPD
Extracellular targeted protein degradation

Advantages of Choosing LifeSensors for your Degrader Drug Discovery

  • Study PROTAC and degrader mediated Ubiquitination and Degradation simultaneously
  • Complete suite of validation studies to establish binding, ternary complex formation, and cellular degradation
  • Experience with novel E3 ligases – ~30 E3 ligases amenable to PROTAC discovery
  • Proteomics to characterize protein degradation – establish selectivity

With deep and diverse expertise in medicinal chemistry, biochemistry, and cell-biology specializing in ubiquitin based drug discovery  for the last 15 years, LifeSensors is proud to offer efficient methods to accelerate your discovery of novel molecules facilitating targeted protein degradation. We offer our degrader discovery services starting from design and synthesis of novel PROTACs, to monitoring PROTAC binding to target and E3 ligases (biochemical and biophysical), including functional ubiquitination and degradation assays in cells. PROTAC-mediated ubiquitylation in vitro permits rapid screening of compound libraries and allows simplification of the medicinal chemistry approach to rationally design potent molecules. Your biochemists can focus on new PROTAC targets as LifeSensors will translate its core technologies for in vitro and cellular PROTAC screens.