Ratiometric Activatable Cell-Penetrating Peptides Provide Rapid In Vivo Readout of Thrombin Activation

被引：89
|
作者：
Whitney, Michael [1 ]
Savariar, Elamprakash N. [1 ]
Friedman, Beth [1 ]
Levin, Rachel A. [1 ]
Crisp, Jessica L. [2 ]
Glasgow, Heather L. [1 ]
Lefkowitz, Roy [1 ]
Adams, Stephen R. [1 ]
Steinbach, Paul [3 ]
Nashi, Nadia [4 ]
Nguyen, Quyen T. [4 ]
Tsien, Roger Y. [1 ,2 ,3 ]
机构：
[1] Univ Calif San Diego, Dept Pharmacol, UCSD Sch Med, La Jolla, CA 92093 USA
[2] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA
[3] Howard Hughes Med Inst, La Jolla, CA USA
[4] Univ Calif San Diego, UCSD Sch Med, Div Otolaryngol Head & Neck Surg, La Jolla, CA 92093 USA
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2013年 / 52卷 / 01期
关键词：
activatable cell-penetrating peptides; FRET; peptides; ratiometric imaging; thrombin; ATHEROSCLEROSIS; INJURY; RECEPTORS; FLUORESCENCE; ISCHEMIA; PLASMIN; CANCER; DAMAGE; BLOOD;
D O I：
10.1002/anie.201205721
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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 (see figure). © 2013 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
引用
收藏
页码：325 / 330
页数：6
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