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Statements

Subject Item
n2:RIV%2F67985858%3A_____%2F09%3A00330745%21RIV10-MSM-67985858
rdf:type
n6:Vysledek skos:Concept
dcterms:description
Mammalian serine racemase (SR) is a pyridoxal-5-phosphate (PLP) dependent enzyme responsible for the biosynthesis of the neurotransmitter d-serine, which activates N-methyl-d-aspartate (NMDA) receptors in the CNS. Aberrant regulation of NMDA receptor signaling has been implicated in a variety of neuropathologies, and inhibitors of SR would therefore be a worthwhile tool for further investigation or treatment of such conditions. Here, we identify a series of small aliphatic hydroxamic acids (HAs) that act as potent SR inhibitors and present a detailed analysis of there mechanism of action. Mammalian serine racemase (SR) is a pyridoxal-5-phosphate (PLP) dependent enzyme responsible for the biosynthesis of the neurotransmitter d-serine, which activates N-methyl-d-aspartate (NMDA) receptors in the CNS. Aberrant regulation of NMDA receptor signaling has been implicated in a variety of neuropathologies, and inhibitors of SR would therefore be a worthwhile tool for further investigation or treatment of such conditions. Here, we identify a series of small aliphatic hydroxamic acids (HAs) that act as potent SR inhibitors and present a detailed analysis of there mechanism of action.
dcterms:title
Hydroxamic acids as a novel family of serine racemase inhibitors: Mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor Hydroxamic acids as a novel family of serine racemase inhibitors: Mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor
skos:prefLabel
Hydroxamic acids as a novel family of serine racemase inhibitors: Mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor Hydroxamic acids as a novel family of serine racemase inhibitors: Mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor
skos:notation
RIV/67985858:_____/09:00330745!RIV10-MSM-67985858
n3:aktivita
n11:Z n11:P
n3:aktivity
P(1M0508), P(IAA400720706), Z(AV0Z40550506), Z(AV0Z40720504)
n3:cisloPeriodika
19
n3:dodaniDat
n12:2010
n3:domaciTvurceVysledku
n18:2658879
n3:druhVysledku
n15:J
n3:duvernostUdaju
n8:S
n3:entitaPredkladatele
n5:predkladatel
n3:idSjednocenehoVysledku
318191
n3:idVysledku
RIV/67985858:_____/09:00330745
n3:jazykVysledku
n16:eng
n3:klicovaSlova
hydroxamic acids; serine racemase; d-serine; pyridoxal-5'-phosphate
n3:klicoveSlovo
n10:hydroxamic%20acids n10:pyridoxal-5%27-phosphate n10:serine%20racemase n10:d-serine
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[883B178129D3]
n3:nazevZdroje
Journal of Medicinal Chemistry
n3:obor
n17:CE
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
6
n3:projekt
n4:IAA400720706 n4:1M0508
n3:rokUplatneniVysledku
n12:2009
n3:svazekPeriodika
52
n3:tvurceVysledku
Cígler, Petr Konvalinka, Jan Šanda, Miloslav Schraml, Jan Hoffman, Hillary Elizabeth Jirásková, Jana
n3:wos
000270361600025
n3:zamer
n7:AV0Z40720504 n7:AV0Z40550506
s:issn
0022-2623
s:numberOfPages
10