論文

査読有り 国際誌
2004年11月26日

Crystal structure of human factor VIIa/tissue factor in complex with peptide mimetic inhibitor

Biochemical and Biophysical Research Communications
  • Shojiro Kadono
  • Akihisa Sakamoto
  • Yasufumi Kikuchi
  • Masayoshi Oh-Eda
  • Naohiro Yabuta
  • Takaki Koga
  • Kunihiro Hattori
  • Takuya Shiraishi
  • Masayuki Haramura
  • Hirofumi Kodama
  • Toru Esaki
  • Haruhiko Sato
  • Yoshiaki Watanabe
  • Susumu Itoh
  • Masateru Ohta
  • Toshiro Kozono
  • 全て表示

324
4
開始ページ
1227
終了ページ
1233
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bbrc.2004.09.182

The 3D structure of human factor VIIa/soluble tissue factor in complex with a peptide mimetic inhibitor, propylsulfonamide-d-Thr-Met-p-aminobenzamidine, is determined by X-ray crystallography. As compared with the interactions between thrombin and thrombin inhibitors, the interactions at S2 and S3 sites characteristic of factor VIIa and factor VIIa inhibitors are revealed. The S2 site has a small pocket, which is filled by the hydrophobic methionine side chain in P2. The small S3 site fits the small size residue, d-threonine in P3. The structural data and SAR data of the peptide mimetic inhibitor show that these interactions in the S2 and S3 sites play an important role for the improvement of selectivity versus thrombin. The results will provide valuable information for the structure-based drug design of specific inhibitors for FVIIa/TF. © 2004 Elsevier Inc. All rights reserved.

リンク情報
DOI
https://doi.org/10.1016/j.bbrc.2004.09.182
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/15504346
Scopus
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=10644283454&origin=inward
Scopus Citedby
https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=10644283454&origin=inward
ID情報
  • DOI : 10.1016/j.bbrc.2004.09.182
  • ISSN : 0006-291X
  • PubMed ID : 15504346
  • SCOPUS ID : 10644283454

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