SPRINTer™ Targeted Protein Degradation Assays

Rapid Cell-based Assays for the Detection of Protein Turnover

Regulated protein degradation is a critical cellular process for endogenous protein homeostasis. Modulating protein turnover by targeting these endogenous pathways is an emerging therapeutic modality referred to as Targeted Protein Degradation (TPD). One modality of TPD uses small molecules such as PROTACs® (Proteolysis Targeting Chimeras) or molecular glues that can redirect the ubiquitin-proteasome mediated degradation pathway and trigger the degradation of specific proteins in a highly selective and effective manner.

This new approach has expanded the druggable target space by allowing drugs to modulate protein turnover or the depletion of over-abundant proteins that have been associated with disease states such as cancer (oncoproteins) or Alzheimer’s Disease (TAU protein).

Eurofins DiscoverX® developed SPRINTer Protein Turnover Biosensor Assays for rapid screening of small molecule therapeutics and quantifying changes in endogenous protein levels in disease-relevant cell models. Detect protein turnover induced by targeted degrader molecules, such as PROTACs, with higher sensitivity and more rapid kinetics than phenotypic endpoint assays (e.g., cell proliferation). Discover new molecular entities that modulate the endogenous levels of targeted proteins by using both SPRINTer platform with InCELL Pulse target engagement assays.

Product Highlights
  • Homogeneous — Simple, scalable, and homogeneous no-wash protocol amenable to high-throughput screening (HTS) formats for increased efficiency
  • Robust & Highly Sensitive – Accurately detect target protein turnover at micro/nanomolar sensitivities
  • Rapid Results — Obtain results in as little as 5 hours to select the right candidate and accelerate development programs
  • Optimized Signal – EFC detection method features lysine-free tags to minimize artifacts

Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.

Products

SPRINTer Protein Turnover Biosensor Cell Lines and eXpress Assay Kits

SPRINTer portfolio includes cell lines and ready-to-use eXpress assay kits featuring cells expressing specific target proteins at physiologically relevant levels. These expression levels are reflective of the physiology of their particular disease model that is crucial for the discovery of disease-relevant therapeutic agents. SPRINTer cell lines, when used along with PathHunter® detection and AssayCompletekits/reagents from Eurofins DiscoverX, can enable detection of drug-induced changes in endogenous cancer targets.

  • SPRINTer Cell Lines – Stable cell lines confirmed for at least 10 passages and rigorously validated for accurate pharmacology
  • SPRINTer eXpress Assay Kits – Complete assay-ready kits with specific cells, optimized reagents, and plates for quick protein turnover assessment

Key Targets:

  • c-Myc, a master regulator during oncogenesis in many cancers such as blood and colon cancer
  • BRD4 (bromodomain), a key transcriptional modulator of c-Myc
  • IKZF1 and IKZF2, an important transcriptional factors in many hematological cancers
  • CDKN1A (p21), a key cell cycle node regulated by numerous proteins, including p53
  • BTK, an important drug target for B-cell related malignancies
  • BRAF(V600E), a common missense mutation across multiple tumor types
  • KRAS(G12C), a common mutation in non-small cell lung cancer, colorectal cancer, and other solid tumors

*PROTAC is a trademark of Arvinas.