A Platform Technology for Accelerated Activation of Fluorescent Probes and Prodrugs

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Invention Summary:

Existing bioimaging and prodrug technologies rely on conventional self-immolative linkers that often suffer from slow or incomplete payload release, resulting in suboptimal imaging contrast or therapeutic index. While inefficient probe activation limits imaging resolution, inadequate drug release poses significant risks: aggressive tumors may continue to proliferate, adapt, develop drug resistance, or actively efflux the prodrug. In addition, probes and prodrugs must cross the plasma membrane of target cells to enable selective intracellular activation. Consequently, conventional probe and prodrug designs often require extensive optimization of polarity and hydrophobicity to achieve sufficient membrane permeability.

Rutgers researchers have developed a novel α-CF₃-benzyl caging/linker platform that significantly accelerates payload release and enhances intracellular availability of the active payload. This chemistry is broadly applicable to aromatic alcohols and enables real-time probe activation, as demonstrated in live-cell studies. This previously unexplored, modular linker design is readily translatable to biochemically triggered imaging probes, existing FDA-approved drugs, and conjugate-based targeted therapeutics.

Market Applications:

• Targeted Therapeutics:
  • Hypoxia-Activated Probes and Prodrugs
  • Protease-Activated Probes and Prodrugs
  • Antibody-Drug and Peptide-Drug Conjugates
• Bioimaging Probes for monitoring intracellular metabolites and redox species

Advantages:

• Accelerated Payload Release Kinetics
• Increased Payload Release Efficacy
• Enhanced Payload Bioavailability
• Broad Compatibility with Fluorophores and Drugs

Publications:

Intellectual Property & Development Status: Provisional application filed. Patent pending. Available for licensing and/or research collaboration. For any business development and other collaborative partnerships, contact:  marketingbd@research.rutgers.edu