Marine natural products as inhibitors of cystathionine beta-synthase activity

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Author list: Thorson MK, Van Wagoner RM, Harper MK, Ireland CM, Majtan T, Kraus JP, Barrios AM
Publisher: Elsevier
Publication year: 2015
Volume number: 25
Issue number: 5
Start page: 1064
End page: 1066
Number of pages: 3
ISSN: 0960-894X
Languages: English-Great Britain (EN-GB)


Abstract

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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Last updated on 2019-23-08 at 11:15