Synthesis and optimization of hyaluronic acid-methotrexate conjugates to maximize benefit in the treatment of osteoarthritis.

@article{Homma2010SynthesisAO,
  title={Synthesis and optimization of hyaluronic acid-methotrexate conjugates to maximize benefit in the treatment of osteoarthritis.},
  author={Akie Homma and Haruhiko Sato and Tatsuya Tamura and Akira Okamachi and Takashi Emura and Takenori Ishizawa and Tatsuya Kato and Tetsu Matsuura and Shigeo Sato and Yoshinobu Higuchi and Tomoyuki Watanabe and Hidetomo Kitamura and Kentaro Asanuma and Tadao Yamazaki and Masahisa Ikemi and Hironoshin Kitagawa and Tadashi Morikawa and Hitoshi Ikeya and Kazuaki Maeda and Koichi Takahashi and Kenji Nohmi and Noriyuki Izutani and Makoto Kanda and Ryohchi Suzuki},
  journal={Bioorganic & medicinal chemistry},
  year={2010},
  volume={18 3},
  pages={1062-75}
}
We previously reported that a conjugate of hyaluronic acid (HA) and methotrexate (MTX) could be a prototype for future osteoarthritis drugs having the efficacy of the two clinically validated agents but with a reduced risk of the systemic side effects of MTX by using HA as the drug delivery carrier. To identify a clinical candidate, we attempted optimization of a lead, conjugate 1. Initially, in fragmentation experiments with cathepsins, we optimized the peptide part of HA-MTX conjugates to be… CONTINUE READING

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