Ratiometric activatable cell-penetrating peptides provide rapid in vivo readout of thrombin activation

Michael Whitney; Elamprakash N Savariar; Beth Friedman; Rachel A Levin; Jessica L Crisp; Heather L Glasgow; Roy Lefkowitz; Stephen R Adams; Paul Steinbach; Nadia Nashi; Quyen T Nguyen; Roger Y Tsien

doi:10.1002/anie.201205721

Ratiometric activatable cell-penetrating peptides provide rapid in vivo readout of thrombin activation

Angew Chem Int Ed Engl. 2013 Jan 2;52(1):325-30. doi: 10.1002/anie.201205721. Epub 2012 Oct 18.

Authors

Michael Whitney¹, Elamprakash N Savariar, Beth Friedman, Rachel A Levin, Jessica L Crisp, Heather L Glasgow, Roy Lefkowitz, Stephen R Adams, Paul Steinbach, Nadia Nashi, Quyen T Nguyen, Roger Y Tsien

Affiliation

¹ Department of Pharmacology, UCSD School of Medicine, University of California San Diego, La Jolla, USA.

Abstract

In real time: thrombin activation in vivo can be imaged in real time with ratiometric activatable cell penetrating peptides (RACPPs). RACPPs are designed to combine 1) dual-emission ratioing, 2) far red to infrared wavelengths for in vivo mammalian imaging, and 3) cleavage-dependent spatial localization. The most advanced RACPP uses norleucine (Nle)-TPRSFL as a linker that increases sensitivity to thrombin by about 90-fold.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Cell-Penetrating Peptides / metabolism*
Fluorescence
Fluorescence Resonance Energy Transfer / methods
Mice
Mice, Transgenic
Thrombin / metabolism*

Substances

Cell-Penetrating Peptides
Thrombin

Abstract

Publication types

MeSH terms

Substances

Grants and funding