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带有靶向载体的双光子不可光解酶抑制剂。

Two-photon uncageable enzyme inhibitors bearing targeting vectors.

作者信息

Anstaett Philipp, Pierroz Vanessa, Ferrari Stefano, Gasser Gilles

机构信息

Department of Chemistry, University of Zurich, Winterthurerstrasse 190, CH-8057 Zurich, Switzerland.

出版信息

Photochem Photobiol Sci. 2015 Oct;14(10):1821-5. doi: 10.1039/c5pp00245a.

DOI:10.1039/c5pp00245a
PMID:26314377
Abstract

The activity of two cyclooxygenase-2 enzyme inhibitors, Celecoxib and Lumiracoxib, could be suppressed by coupling to photo-labile protecting groups, so-called photocages. These groups could be further functionalized with a peptide targeting vector for specific cellular delivery. The enzyme inhibition potential of the cyclooxygenase-2 inhibitors could be regained upon two-photon excitation with tissue-transparent near-IR light at 800 nm.

摘要

两种环氧化酶-2(COX-2)酶抑制剂塞来昔布和鲁米昔布的活性可通过与光不稳定保护基团(即所谓的光笼)偶联而被抑制。这些基团可用靶向肽载体进一步功能化,以实现特定的细胞递送。在800 nm的组织透明近红外光双光子激发下,环氧化酶-2抑制剂的酶抑制潜力得以恢复。

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Two-photon uncageable enzyme inhibitors bearing targeting vectors.带有靶向载体的双光子不可光解酶抑制剂。
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