Development of functionalized peptides for efficient inhibition of myostatin by selective photooxygenation,Organic & Biomolecular Chemistry

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Development of functionalized peptides for efficient inhibition of myostatin by selective photooxygenation
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-11-03 , DOI: 10.1039/d0ob02042g
Hideyuki Okamoto ₁ , Atsuhiko Taniguchi , Shoya Usami , Masahiro Katsuyama , Sho Konno , Akihiro Taguchi , Kentaro Takayama , Yoshio Hayashi

Affiliation

For the inhibition of myostatin, which is an attractive strategy for the treatment of muscle atrophic disorders including muscular dystrophy, myostatin-binding peptides were synthesized with an on/off-switchable photooxygenation catalyst at different positions on the peptide chain. These functionalized peptides oxygenated and inactivated myostatin upon irradiation with near-infrared light. Among the peptides tested, a peptide (5) with the catalyst moiety at the 16 position induced myostatin-selective photooxygenation, and efficiently inhibited myostatin. These peptides exhibited low phototoxicity. Such functionalized peptides would provide a precedented strategy for myostatin-targeting therapy, in which myostatin is irreversibly and catalytically inactivated by photooxygenation.

中文翻译：

开发通过选择性光氧化有效抑制肌生长抑制素的功能化肽

为了抑制肌生长抑制素，这是一种治疗包括肌肉营养不良在内的肌肉萎缩性疾病的有吸引力的策略，通过在肽链的不同位置上开/关可切换的光氧化催化剂合成了肌生长抑制素结合肽。这些功能化的肽在用近红外光照射后氧化并失活了肌肉生长抑制素。在所测试的肽中，具有在16位的催化剂部分的肽（5）诱导了肌生成抑制素选择性的光氧化作用，并有效地抑制了肌生成抑制素。这些肽表现出低的光毒性。此类功能化的肽将为肌肉生长抑制素靶向治疗提供先例策略，其中肌肉生长抑制素通过光氧化作用不可逆地和催化失活。

更新日期：2020-11-12

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