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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Author(s): S. Kadono, A. Sakamoto, Y. Kikuchi, M. Oh-eda, N. Yabuta, T. Koga, K. Hattori, T. Shiraishi, M. Haramura and H. Kodama

Volume 2, Issue 3, 2005

Page: [177 - 181] Pages: 5

DOI: 10.2174/1570180053765200

Price: $65

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.

Keywords: factor vIIa, blood coagulation, antithrombotic, serine protease, x-ray crystallography, drug design


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