Target intelligence / Profile preview

Serine racemase (SR)

Target
SR
Molecular classification
Enzyme, Pyridoxal phosphate-dependent enzyme, Racemase
01

Overview

Serine racemase is a pyridoxal 5'-phosphate-dependent enzyme found in humans and encoded by the SRR gene. It catalyzes the racemization of L-serine to D-serine, a process crucial for producing D-serine, which acts as an important co-agonist of NMDA receptors in the central nervous system. Serine racemase also catalyzes the β-elimination of L-serine to pyruvate and ammonia, a pathway that can divert L-serine from D-serine production. The enzyme is allosterically regulated by ATP and divalent cations, and its function is critical for modulating glutamatergic neurotransmission. Dysregulation of serine racemase or D-serine levels is associated with neuropsychiatric disorders such as schizophrenia and may play a role in neurodegeneration and acute brain injuries like ischemic stroke. While there are no approved drugs directly targeting serine racemase, D-serine (the product of the enzyme) is under clinical investigation for a variety of psychiatric and neurological disorders

Other names
SRSRRserine racemase (human)EC 5.1.1.18
02

Mechanism of action

Inhibition of serine racemase reduces D-serine synthesis, lowering NMDA receptor co-activation Activation or increased expression augments D-serine production, enhancing NMDA receptor function

03

Biological functions

Catalyzes racemization of L-serine to D-serineβ-elimination of L-serine to pyruvate and ammoniaRegulation of D-serine levels in the central nervous systemModulation of NMDA (N-methyl-D-aspartate) receptor signaling
04

Disease associations

Neurodegenerative disease (dysregulation linked to neurodegeneration)Schizophrenia (NMDA receptor hypofunction hypothesis)Ischemic stroke (neuronal infarction)
05

Safety considerations

Excessive inhibition could reduce D-serine, impair NMDA receptor function (potential cognitive/psychiatric side effects)Excessive activation could elevate D-serine, risking neurotoxicity via NMDA receptor overactivationAs with other central nervous system targets, potential for off-target neurological and psychiatric effects
06

Interacting drugs

No approved direct inhibitors or activators are on the market; however, D-serine (the product) is used as a therapeutic in schizophrenia

1 more in the full profile.

07

Biomarkers

SRR gene/protein expression and activity in brain tissue (research use)D-serine levels in cerebrospinal fluid or brain (as indirect indicator of SR function and NMDA pathway activity)

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