Fast Acting Molecular Probes for Real-Time In Vivo Study of Disease and Therapeutics

This technology is for fast acting molecular probes made from a fluorescent quencher molecule, a fluorophore, an enzyme cleavable oligopeptide (for example targeted by protease) and FDA-approved polyethylene glycol (PEG) as well as associated methods to identify cell activity with these probes. Proteases regulate many cell processes such as inflammation as well as pathological processes in cancer and cardiovascular disease. High protease activity is associated with metastatic cancers. Proteases are also active in apoptosis, and tissue remodeling in cardiovascular disease. Although highly useful in vitro, conventional probes are unstable, nonspecific or slow activating in vivo. This new probe is faster than standard probes (30 min vs. 24 hrs) and has enhanced target-to background ratios. It enables quick screening of animals in an array of applications related to protease-associated diseases and other diseases. It may detect specific biological targets and monitor in vivo therapeutic efficacy in real time. Most drug candidates identified by in vitro screening fail in vivo. Failures are costly. Identifying in vivo drug efficacy sooner would reduce waste and increase successful drug development.

Potential Commercial Applications: Competitive Advantages:
  • Diagnostics
  • In vivo therapeutic monitoring
  • Faster than standard probes
  • Enhanced target-to-background ratios
  • Allows in vivo therapeutic efficacy study in real time

Development Stage:
  • Early-stage
  • Pre-clinical
  • In vivo data available (animal)


Xiaoyuan Chen (NIBIB)  ➽ more inventions...

Seulki Lee (NIBIB)  ➽ more inventions...

Lei Zhu (NIBIB)  ➽ more inventions...

Intellectual Property:
US Pat: 10,646,591 issued 2020-05-12
US Application No. 61/533,014 filed on 2011-09-09
PCT Application No. PCT/US2012/054121 filed on 2012-09-07
US Application No. 14/343,469 filed on 2014-05-01


Lee S, et al.

PMID 19842672

Lee S, et al.

PMID 20388112

Collaboration Opportunity:

The National Institute of Biomedical Imaging and Bioengineering is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize fast acting molecular probes for real-time in vivo study of disease and therapeutics. For collaboration opportunities, please contact Cecilia Pazman at pazmance@nhlbi.nih.

Licensing Contact:
Michael Shmilovich, J.D.
Phone: 301-435-5019

OTT Reference No: E-079-2011-0
Updated: Feb 12, 2015