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PreprintCC BY-NC-NDChemRxiv

Molecular rotor-regulated target-selective photoinactivation of myostatin

  • Kaoru Ikekawa1
  • Hideyuki Okamoto1,2
  • Shuko Amber Murano1
  • Jo Yamamoto1
  • Kota Inada1
  • Sho Konno1
  • Akihiro Taguchi1
  • Hikaru Yanai3
  • Yoichi Negishi2
  • Yoshio Hayashi1
  • Atsuhiko Taniguchi1
  1. 1Laboratory of Medicinal Chemistry, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo, Japan, 192-0392
  2. 2Laboratory of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo, Japan, 192-0392
  3. 3Laboratory of Synthetic Organic Chemistry, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo , Japan, 192-0392
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Abstract

Photoinactivation allows precise spatiotemporal control of biomolecules in biological systems. Among the photoinactivation strategies, photooxygenation is advantageous, as it can be readily induced with a photosensitizer upon photoirradiation in biological environment. However, its utility is limited by poor target selectivity arising from the excessive generation and high reactivity of reactive oxygen species. Here, target-selective photoinactivation of myostatin is achieved using a target-binding ligand functionalized with a molecular rotor-based photosensitizing unit whose photooxygenation activity is enhanced upon binding to the target protein. A novel molecular rotor-based photosensitizer was developed and conjugated to a myostatin-binding peptide. The resulting functionalized peptide selectively oxygenated and inactivated myostatin under near-infrared irradiation. Treatment with the peptide followed by irradiation decreased endogenous myostatin levels in skeletal muscle, leading to increased muscle weight and muscle fiber size. This target-selective photoinactivation strategy may expand the applicability of photoresponsive approaches for the treatment of various diseases, including muscular dystrophy.

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Cite

BibTeXRIS
BibTeX
@misc{ikekawa2026molecular,
  title = {{Molecular rotor-regulated target-selective photoinactivation of myostatin}},
  author = {Kaoru Ikekawa and Hideyuki Okamoto and Shuko Amber Murano and Jo Yamamoto and Kota Inada and Sho Konno and Akihiro Taguchi and Hikaru Yanai and Yoichi Negishi and Yoshio Hayashi and Atsuhiko Taniguchi},
  howpublished = {ChemRxiv},
  year = {2026},
  month = sep,
  doi = {10.26434/chemrxiv.15008871/v1},
  url = {https://chemrxiv.org/doi/full/10.26434/chemrxiv.15008871/v1},
  note = {CC BY-NC-ND},
}
RIS
TY  - UNPB
TI  - Molecular rotor-regulated target-selective photoinactivation of myostatin
AU  - Kaoru Ikekawa
AU  - Hideyuki Okamoto
AU  - Shuko Amber Murano
AU  - Jo Yamamoto
AU  - Kota Inada
AU  - Sho Konno
AU  - Akihiro Taguchi
AU  - Hikaru Yanai
AU  - Yoichi Negishi
AU  - Yoshio Hayashi
AU  - Atsuhiko Taniguchi
PY  - 2026
DA  - 2026/09/15
PB  - ChemRxiv
DO  - 10.26434/chemrxiv.15008871/v1
UR  - https://chemrxiv.org/doi/full/10.26434/chemrxiv.15008871/v1
AB  - Photoinactivation allows precise spatiotemporal control of biomolecules in biological systems. Among the photoinactivation strategies, photooxygenation is advantageous, as it can be readily induced with a photosensitizer upon photoirradiation in biological environment. However, its utility is limited by poor target selectivity arising from the excessive generation and high reactivity of reactive oxygen species. Here, target-selective photoinactivation of myostatin is achieved using a target-binding ligand functionalized with a molecular rotor-based photosensitizing unit whose photooxygenation activity is enhanced upon binding to the target protein. A novel molecular rotor-based photosensitizer was developed and conjugated to a myostatin-binding peptide. The resulting functionalized peptide selectively oxygenated and inactivated myostatin under near-infrared irradiation. Treatment with the peptide followed by irradiation decreased endogenous myostatin levels in skeletal muscle, leading to increased muscle weight and muscle fiber size. This target-selective photoinactivation strategy may expand the applicability of photoresponsive approaches for the treatment of various diseases, including muscular dystrophy.
ER  -