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

页码：325 / 330

页数：6

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