Extending the Half-Life of a Protein in Vivo by Enzymatic Labeling with Amphiphilic Lipopeptides

Mari Takahara, Shinichi Mochizuki, Rie Wakabayashi, Kosuke Minamihata, Masahiro Goto, Kazuo Sakurai, Noriho Kamiya

研究成果: ジャーナルへの寄稿学術誌査読

7 被引用数 (Scopus)


Synthesis of lipid-protein conjugates is one of the significant techniques in drug delivery systems of proteins; however, the intact conjugation of a lipid and protein is yet challenging due to the hydrophobicity of lipid molecules. In order to facilitate easy handling of the lipid moiety in conjugation, we have focused on a microbial transglutaminase (MTG) that can ligate specific lysine (K) and glutamine (Q) residues in lipopeptides and a protein of interest. As MTG substrates, monolipid- and dilipid-fused amphiphilic short lipopeptide substrates (lipid-G3S-RHK or lipid2-KG3S-RHK) were designed. These amphiphilic lipopeptides and a model protein (enhanced green fluorescent protein, EGFP) fused with LLQG (LQ-EGFP) were both water-soluble, and thus lipid-protein conjugates were efficiently obtained through the MTG reaction with a >80% conversion rate of LQ-EGFP even using cholesterol-G3S-RHK. In vitro cell adhesion and in vivo half-life stability of the successfully obtained lipid-protein conjugates were evaluated, showing that the monocholesterol-G3S-RHK modification of a protein gave the highest cell adhesion efficiency and longest half-life time by formation of a stable albumin/lipid-protein complex.

ジャーナルBioconjugate Chemistry
出版ステータス出版済み - 4月 21 2021

!!!All Science Journal Classification (ASJC) codes

  • バイオテクノロジー
  • バイオエンジニアリング
  • 生体医工学
  • 薬理学
  • 薬科学
  • 有機化学


「Extending the Half-Life of a Protein in Vivo by Enzymatic Labeling with Amphiphilic Lipopeptides」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。