期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 15, 页码 4126-4129出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.013
关键词
Thrombin; Factor Xa; Inhibition; Allosteric; Synthetic small molecules; Library; Screening; Lignins; Dehydropolymers
资金
- National Heart, Lung and Blood Institute [HL069975, HL090586]
- American Heart Association National Center [EIA 0640053N]
- A. D. Williams Foundation [6-46064]
- Mizutani Foundation for Glycoscience
Designing non-saccharide functional mimics of heparin is a major challenge. In this work, a library of small, aromatic molecules based on the sulfated DHP scaffold was synthesized and screened against thrombin and factor Xa. The results reveal that (i) selected monomeric benzofuran derivatives inhibit the two enzymes, albeit weakly; (ii) the two enzymes recognize different structural features in the benzofurans studied suggesting significant selectivity of recognition; and (iii) the mechanism of inhibition is allosteric. The molecules represent the. first allosteric small molecule inhibitors of the two enzymes. (C) 2009 Elsevier Ltd. All rights reserved.
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