期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 5, 页码 1064-1066出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.01.013
关键词
Hydrogen sulfide; Sulfur metabolism; Fluorogenic probe; Inhibitor screen
资金
- American Heart Association [11GRNT7530023]
- National Institutes of Health [CA36622]
A library consisting of characterized marine natural products as well as synthetic derivatives was screened for compounds capable of inhibiting the production of hydrogen sulfide (H2S) by cystathionine beta- synthase (CBS). Eight hits were validated and shown to inhibit CBS activity with IC50 values ranging from 83 to 187 mu M. The majority of hits came from a series of synthetic polyandrocarpamine derivatives. In addition, a modified fluorogenic probe for H2S detection with improved solubility in aqueous solutions is reported. (C) 2015 Elsevier Ltd. All rights reserved.
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