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Bioorg Med Chem Lett. 2015 Mar 1;25(5):1064-6. doi: 10.1016/j.bmcl.2015.01.013. Epub 2015 Jan 14.

Marine natural products as inhibitors of cystathionine beta-synthase activity.

Author information

1
Department of Medicinal Chemistry, University of Utah, 30 South 2000 East, Salt Lake City, UT 84112, USA.
2
Department of Pediatrics, University of Colorado, Aurora, CO 80045, USA.
3
Department of Medicinal Chemistry, University of Utah, 30 South 2000 East, Salt Lake City, UT 84112, USA. Electronic address: amy.barrios@utah.edu.

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.

KEYWORDS:

Fluorogenic probe; Hydrogen sulfide; Inhibitor screen; Sulfur metabolism

PMID:
25666819
DOI:
10.1016/j.bmcl.2015.01.013
[Indexed for MEDLINE]

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