Marine natural products as inhibitors of cystathionine beta-synthase activity

作者：Thorson Megan K; Van Wagoner Ryan M; Harper Mary Kay; Ireland Chris M; Majtan Tomas; Kraus Jan P; Barrios Amy M^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(5): 1064-1066.

DOI：10.1016/j.bmcl.2015.01.013

• Hydrogen sulfide
• Sulfur metabolism
• Fluorogenic probe
• Inhibitor screen

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.

• 出版日期2015-3-1