Peptide Mimetic Factor VIIa Inhibitor: Importance of Hydrophilic Pocket in S2 Site to Improve Selectivity Against Thrombin

S. Kadono; A. Sakamoto; Y. Kikuchi; M. Oh-eda; N. Yabuta; T. Koga; K. Hattori; T. Shiraishi; M. Haramura; H. Kodama

doi:10.2174/1570180053765200

ISSN: 1570-1808
E-ISSN: 1875-628X

Peptide Mimetic Factor VIIa Inhibitor: Importance of Hydrophilic Pocket in S2 Site to Improve Selectivity Against Thrombin
Authors: S. Kadono¹, A. Sakamoto², Y. Kikuchi³, M. Oh-eda⁴, N. Yabuta⁵, T. Koga⁶, K. Hattori⁷, T. Shiraishi⁸, M. Haramura⁹ and H. Kodama¹⁰
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¹ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ² Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ³ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ⁴ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ⁵ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ⁶ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ⁷ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ⁸ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ⁹ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. ¹⁰ Fuji Gotemba Research Labs, Chugai Pharmaceutical Co., Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan.
Source: Letters in Drug Design & Discovery, Volume 2, Issue 3, May 2005, p. 177 - 181
DOI: https://doi.org/10.2174/1570180053765200
- Available online: 01 May 2005

Abstract

X-ray structure analysis of human factor VIIa/soluble tissue factor in complex with a peptide mimetic inhibitor reveals that Asp60, Tyr94, and Thr98 in the S2 site play an important role for the improvement of selectivity against thrombin.

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2005-05-01

2025-05-29

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Article Type: Review Article

Keyword(s): antithrombotic; blood coagulation; drug design; factor vIIa; serine protease; x-ray crystallography

Peptide Mimetic Factor VIIa Inhibitor: Importance of Hydrophilic Pocket in S2 Site to Improve Selectivity Against Thrombin

Abstract

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