Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5′-phosphate …

HE Hoffman, J Jirásková, P Cígler…

Index: Hoffman, Hillary E.; Jiraskova, Jana; Cigler, Petr; Sanda, Miloslav; Schraml, Jan; Konvalinka, Jan Journal of Medicinal Chemistry, 2009 , vol. 52, # 19 p. 6032 - 6041

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Citation Number: 24

Abstract

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 ...