Marine Natural Products As Inhibitors of Cystathionine Beta-Synthase Activity
Bioorganic & Medicinal Chemistry Letters（2015）
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 187μM. 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.
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Key words
Hydrogen sulfide,Sulfur metabolism,Fluorogenic probe,Inhibitor screen
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