4.5 Article

Marine natural products as inhibitors of cystathionine beta-synthase activity

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

  1. American Heart Association [11GRNT7530023]
  2. National Institutes of Health [CA36622]

向作者/读者索取更多资源

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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