RGD Reference Report - Development of LC/MS/MS, high-throughput enzymatic and cellular assays for the characterization of compounds that inhibit kynurenine monooxygenase (KMO). - Rat Genome Database

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Development of LC/MS/MS, high-throughput enzymatic and cellular assays for the characterization of compounds that inhibit kynurenine monooxygenase (KMO).

Authors: Winkler, Dirk  Beconi, Maria  Toledo-Sherman, Leticia M  Prime, Michael  Ebneth, Andreas  Dominguez, Celia  Muñoz-Sanjuan, Ignacio 
Citation: Winkler D, etal., J Biomol Screen. 2013 Sep;18(8):879-89. doi: 10.1177/1087057113489731. Epub 2013 May 20.
RGD ID: 13513904
Pubmed: (View Article at PubMed) PMID:23690293
DOI: Full-text: DOI:10.1177/1087057113489731

Kynurenine monooxygenase (KMO) catalyzes the conversion of kynurenine to 3-hydroxykynurenine. Modulation of KMO activity has been implicated in several neurodegenerative diseases, including Huntington disease. Our goal is to develop potent and selective small-molecule KMO inhibitors with suitable pharmacokinetic characteristics for in vivo proof-of-concept studies and subsequent clinical development. We developed a comprehensive panel of biochemical and cell-based assays that use liquid chromatography/tandem mass spectrometry to quantify unlabeled kynurenine and 3-hydroxykynurenine. We describe assays to measure KMO inhibition in cell and tissue extracts, as well as cellular assays including heterologous cell lines and primary rat microglia and human peripheral blood mononuclear cells.



Gene Ontology Annotations    

Biological Process

Objects Annotated

Genes (Rattus norvegicus)
Kmo  (kynurenine 3-monooxygenase)


Additional Information