Počet záznamů: 1

Hydroxamic acids as a novel family of serine racemase inhibitors: Mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor

  1. 1.
    0330745 - UOCHB-X 2010 RIV US eng J - Článek v odborném periodiku
    Hoffman, Hillary Elizabeth - Jirásková, Jana - Cígler, Petr - Šanda, Miloslav - Schraml, Jan - Konvalinka, Jan
    Hydroxamic acids as a novel family of serine racemase inhibitors: Mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor.
    Journal of Medicinal Chemistry. Roč. 52, č. 19 (2009), s. 6032-6041 ISSN 0022-2623
    Grant CEP: GA MŠk 1M0508; GA AV ČR IAA400720706
    Výzkumný záměr: CEZ:AV0Z40550506; CEZ:AV0Z40720504
    Klíčová slova: hydroxamic acids * serine racemase * d-serine * pyridoxal-5'-phosphate
    Kód oboru RIV: CE - Biochemie
    Impakt faktor: 4.802, rok: 2009

    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.
    Trvalý link: http://hdl.handle.net/11104/0176459