Development of Novel Diagnostic Agents for Atherosclerosis Using Fluorescence-labeled Peptides

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  • 蛍光標識ペプチドを用いた新規動脈硬化診断薬の開発研究
  • ケイコウ ヒョウシキ ペプチド オ モチイタ シンキ ドウミャク コウカ シンダンヤク ノ カイハツ ケンキュウ

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Abstract

 The oxidative modification of low-density lipoprotein (LDL) is believed to play an important role in the pathogenesis of atherosclerosis. Therefore, probes for detection of oxidized LDL (ox-LDL) in atherosclerotic plaques and plasma are expected to be useful for the diagnosis of atherosclerosis. Recently, we found that four fluorescein isothiocyanate (FITC)-labeled heptapeptides (Lys-Trp-Tyr-Lys-Asp-Gly-Asp, KP6)—(FITC)KP6 and (FITC-AC)KP6— and then substitution with D-Lys at the N-terminus—(FITC)dKP6 and (FITC-AC)dKP6— bind with high specificity and high affinity to two oxidized forms of LDL, heavily oxidized LDL and minimally modified LDL (MM-LDL), through binding to lysophosphatidylcholine and oxidized phosphatidylcholine, present abundantly in heavily oxidized LDL and MM-LDL. Moreover, (FITC)dKP6 and (FITC-AC)dKP6 were more stable than (FITC)KP6 and (FITC-AC)KP6 in plasma in vitro. (FITC)KP6 could detect foam cells in atherosclerotic aortic plaques of apoE-knockout mice. These results suggest that four fluorescence-labeled heptapeptides could be efficient fluorescent probes for the specific detection of ox-LDL, and can therefore contribute to the identification, diagnosis, prevention, and treatment of atherosclerosis.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 136 (10), 1367-1372, 2016-10-01

    The Pharmaceutical Society of Japan

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