Discovery of Depsides and Depsidones from Lichen as Potent Inhibitors of Microsomal Prostaglandin E2 Synthase‐1 Using Pharmacophore Models | Zendy

Bauer Julia | Zendy; Waltenberger Birgit | Zendy; Noha Stefan M. | Zendy; Schuster Daniela | Zendy; Rollinger Judith M. | Zendy; Boustie Joel | Zendy; Chollet Marylene | Zendy; Stuppner Hermann | Zendy; Werz Oliver | Zendy

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Discovery of Depsides and Depsidones from Lichen as Potent Inhibitors of Microsomal Prostaglandin E2 Synthase‐1 Using Pharmacophore Models

Author(s) -

Bauer Julia,

Waltenberger Birgit,

Noha Stefan M.,

Schuster Daniela,

Rollinger Judith M.,

Boustie Joel,

Chollet Marylene,

Stuppner Hermann,

Werz Oliver

Publication year - 2012

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.201200345

Subject(s) - pharmacophore , virtual screening , in silico , chemistry , stereochemistry , computational biology , biochemistry , biology , gene

Nature in silico: Virtual screening using validated pharmacophore models identified lichen depsides and depsidones as potential inhibitors of mPGES‐1, an emerging target for NSAIDs. Evaluation of the virtual hits in a cell‐free assay revealed physodic acid and perlatolic acid as potent inhibitors of mPGES‐1 (IC 50 = 0.4 and 0.43 μ M , respectively), indicating that these natural products have potential as novel anti‐inflammatory agents.

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