Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.5.1.4 (deaminase)
 5,113 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The pineal aryl acylamidase (AAA) activity has been demonstrated and characterized for the first time using ONAc as a substrate. The pineal AAA activity in the presence of 0.05% Triton X-100 was linear with protein concentration up to 1 mg and with incubation time up to 1 hour. Both the rat and bovine pineal showed a pH optimum at 5.0. The in vitro and in vivo effects of several classes of drugs on the pineal AAA activity were examined. At 0.1 mM, 5-HT, N-acetyl-5HT, melatonin, d-LSD, l-LSD, methiothepin, DA, chlorimipramine, imipramine, pargyline, TH C and harmaline significantly inhibited the rat pineal AAA activity by 19-51%. N-Acetyl-5-HT was the most potent in vitro inhibitor. However, at the same concentration, NE, 6-MeO-harman and eserine did not show any effect on the enzyme activity. Lineweaver-Burk plot indicated a competitive type of in vitro inhibition of the pineal AAA activity by melatonin. Acute subcutaneous injection of low doses (25-50 mg/kg) THBC harmaline, desipramine and protriptyline markedly inhibited the rat pineal AAA activity but at higher doses (75-100 mg/kg) the inhibition was reduced. On the contrary, RO4-4602 (200-800 mg/kg) greatly enhanced (1.5-2.3 fold) the enzyme activity, inversely proportional to the doses given. In view of the differential effects of these drugs on the brain and pineal AAA, it seems unlikely that they would be the same enzyme.
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PMID:Pineal aryl acylamidase: effects of melatonin, serotonin-related compounds, beta-carbolines, RO4-4602 and antidepressants. 670 61

1. The serotonin (5-HT) sensitive brain aryl acylamidase (AAA) has received considerable attention due to its potential involvement in 5-HT action mechanism in CNS. 2. Multiple forms, AAA-1 and 2, have been separated by ammonium sulfate precipitation of brain extract and subsequent gel filtration. 3. Their chemical properties have been characterized and differentiated by effects of several classes of drugs including d-LSD, 5-HT, 5-HT related compounds and tetrahydro-beta-carbolines on their enzyme activities. 4. In the rat brain, AAA-1 shows highest specific activity in corpus striatum and lowest activity in cerebellum whereas AAA-2 shows highest specific activity in cerebellum and lowest activity in corpus striatum. 5. Subcellularly, AAA-1 exhibits highest specific activity in synaptosomal fraction of rat corpus striatum, lowest activity in mitochondrial fraction and no activity in nuclear fraction while AAA-2 exhibits highest specific activity in microsomal fraction and lowest activity in nuclear fraction. 6. Triton X-100 treatment altered the subcellular distribution pattern of both AAA-1 and AAA-2. 7. AAA-2 is possibly associated with true acetylcholinesterase (AChE) in brain based on its inhibition by neostigmine but its identity with AChE needs further elucidation. 8. To determine the physiological role(s) for brain AAA, naturally occurring aromatic alkylamines other than melatonin need to be tested as possible substrate(s) for the enzyme activity.
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PMID:Brain aryl acylamidase. 675 8