About: Selective and competitive inhibition of kynurenine aminotransferase 2 by glycyrrhizic acid and its analogues

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About: Selective and competitive inhibition of kynurenine aminotransferase 2 by glycyrrhizic acid and its analogues Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Selective and competitive inhibition of kynurenine aminotransferase 2 by glycyrrhizic acid and its analogues
Creator	Fujigaki, Hidetsugu Fujigaki, Suwako Kato, Koichi Kunisawa, Kazuo Mouri, Akihiro Oda, Akifumi Saito, Kuniaki Yamamoto, Yasuko Yamazaki, Kyoka Yoshida, Yukihiro
Source	PMC
abstract	The enzyme kynurenine aminotransferase (KAT) catalyses the conversion of kynurenine (KYN) to kynurenic acid (KYNA). Although the isozymes KAT1–4 have been identified, KYNA is mainly produced by KAT2 in brain tissues. KNYA is an antagonist of N-methyl-D-aspartate and α-7-nicotinic acetylcholine receptors, and accumulation of KYNA in the brain has been associated with the pathology of schizophrenia. Therefore, KAT2 could be exploited as a therapeutic target for the management of schizophrenia. Although currently available KAT2 inhibitors irreversibly bind to pyridoxal 5′-phosphate (PLP), inhibition via this mechanism may cause adverse side effects because of the presence of other PLP-dependent enzymes. Therefore, we identified novel selective KAT2 inhibitors by screening approximately 13,000 molecules. Among these, glycyrrhizic acid (GL) and its analogues, glycyrrhetinic acid (GA) and carbenoxolone (CBX), were identified as KAT2 inhibitors. These compounds were highly selective for KAT2 and competed with its substrate KYN, but had no effects on the other 3 KAT isozymes. Furthermore, we demonstrated that in complex structures that were predicted in docking calculations, GL, GA and CBX were located on the same surface as the aromatic ring of KYN. These results indicate that GL and its analogues are highly selective and competitive inhibitors of KAT2.
has issue date	2019-07-15(xsd:dateTime)
bibo:doi	10.1038/s41598-019-46666-y
bibo:pmid	31308447
has license	cc-by
sha1sum (hex)	5080b4cb5df826f641dc6602e27dcca510ccada8
schema:url	https://doi.org/10.1038/s41598-019-46666-y
resource representing a document's title	Selective and competitive inhibition of kynurenine aminotransferase 2 by glycyrrhizic acid and its analogues
has PubMed Central identifier	PMC6629613
has PubMed identifier	31308447
schema:publication	Sci Rep
resource representing a document's body	covid:5080b4cb5df826f641dc6602e27dcca510ccada8#body_text
is schema:about of	named entity 'REGULATORY' named entity 'demonstrated' named entity 'compounds' named entity 'kynurenine' named entity 'molecules' named entity 'selective' named entity 'therapeutic' named entity 'pyridoxal' named entity 'Graduate School' named entity 'HEALTH' named entity 'DEPARTMENT' named entity 'SCIENCE' named entity 'CONVERSION' named entity 'PREDICTED' named entity '80%' named entity 'RESULTS' named entity 'BRAIN TISSUES' named entity 'OTHER 3' named entity 'THE BRAIN' named entity 'KYNURENIC ACID' named entity 'AVAILABLE' named entity 'KYNA' named entity 'N-METHYL-D-ASPARTATE' named entity 'MANAGEMENT' named entity 'KAT' named entity 'GLYCYRRHETINIC ACID' named entity 'ENZYME' named entity 'KYNURENINE' named entity 'KAT2' named entity 'PLP' named entity 'GRADUATE SCHOOL' named entity 'SELECTIVE' named entity 'NOVEL' named entity 'JAPAN' named entity 'UNIVERSITY' named entity 'HEALTH SCIENCES' named entity 'IDENTIFIED' named entity 'INHIBITORS' named entity 'EFFECTS' named entity 'SCREENING' named entity 'MOLECULES' named entity 'KYNURENINE AMINOTRANSFERASE' named entity 'BUT' named entity 'CATALYSES' named entity 'NICOTINIC ACETYLCHOLINE RECEPTORS' named entity 'ASSOCIATED WITH' named entity 'SUBSTRATE' named entity 'THESE' named entity 'CARBENOXOLONE' named entity 'ISOZYMES' named entity 'PATHOLOGY' named entity 'STRUCTURES' named entity 'GLYCYRRHIZIC ACID' named entity 'KAT1' named entity 'APPROXIMATELY' named entity 'ACCUMULATION' named entity 'SIDE EFFECTS' named entity 'HAVE' named entity 'CAUSE' named entity 'ITS' named entity 'COMPLEX' named entity 'SURFACE' named entity 'AROMATIC RING' named entity 'KYN' named entity 'BIND' named entity 'MECHANISM' named entity 'CBX' named entity 'COMPETITIVE INHIBITORS' named entity 'COULD BE' named entity 'SCHIZOPHRENIA' named entity 'THERAPEUTIC TARGET' named entity 'INHIBITION'

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