Transaminase inhibitor

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A transaminase inhibitor (synonymous aminotransferase inhibitor ) is an inhibitor of aminotransferases .


Examples of transaminase inhibitors are the GABA transaminase inhibitor vigabatrin , γ-acetylene-GABA, ethanolamine-O-sulfate, aminoxyacetic acid, gabaculin and valproic acid , which is used in the treatment of epilepsy , bipolar disorders and migraines . The transaminase inhibitor 4- (4-fluorophenoxy) benzaldehyde semicarbazone (C0102862, V102862) serves as a lead structure in the development of anticonvulsants due to its effect as a sodium channel inhibitor and GABA transaminase inhibitor .

The main vector of malaria , Anopheles gambiae , has an atypical transaminase ( 3-hydroxy- kynurenine transaminase ), the selective inhibition of which is being investigated for use in insecticides or as a result to interrupt the chain of malaria infections .

Web links

Individual evidence

  1. Lippert, B., Metcalf, BW, Jung, MJ and Casara, P .: 4-aminohex-5-enoic acid, a selective catalytic inhibitor of 4-aminobutyrate aminotransferase in mammalian brain. European Journal of Biochemistry No. 74, p. 441 (1977).
  2. Jung, MJ, Lippert, B., Metcalf, BW, Schechter, PJ, Böhlen, P. and Sjoerdsma, A .: The effect of 4-amino-hex-5-ynoic acid (γ-acetylenic GABA, γ-ethynyl GABA), a catalytic inhibitor of GABA transaminase, on brain GABA metabolism. Journal of Neurochemistry No. 28 p. 717 (1977).
  3. ^ A b D. G. Grahame-Smith: Preclinical Psychopharmacology Part 1 , Elsevier, 2013, ISBN 978-1-4832-7533-8 , pp. 124, 129.
  4. ^ A b R. Bernasconi, L. Maitre, P. Martin, F. Raschdorf: The use of inhibitors of GABA-transaminase for the determination of GABA turnover in mouse brain regions: an evaluation of aminooxyacetic acid and gabaculine. In: Journal of neurochemistry. Volume 38, Number 1, January 1982, ISSN  0022-3042 , pp. 57-66, PMID 7108535 .
  5. P. Zwanzger, TC Baghai, C. Schuele, A. Ströhle, F. Padberg, N. Kathmann, M. Schwarz, HJ Möller, R. Rupprecht: Vigabatrin decreases cholecystokinin-tetrapeptide (CCK-4) induced panic in healthy volunteers . In: Neuropsychopharmacology . Volume 25, Number 5, November 2001, ISSN  0893-133X , pp. 699-703, doi : 10.1016 / S0893-133X (01) 00266-4 , PMID 11682253 .
  6. SN Pandeya: Semicarbazone - a versatile therapeutic pharmacophore for fragment based anticonvulsant drug design. In: Acta Pharmaceutica . Volume 62, Number 3, November 2012, ISSN  1846-9558 , pp. 263-286, doi: 10.2478 / v10007-012-0030-1 , PMID 23470343 .
  7. F. Rossi, F. Lombardo, A. Paglino, C. Cassani, G. Miglio, B. Arcà, M. Rizzi: Identification and biochemical characterization of the Anopheles gambiae 3-hydroxykynurenine transaminase. In: FEBS Journal . Volume 272, Number 21, November 2005, ISSN  1742-464X , pp. 5653-5662, doi: 10.1111 / j.1742-4658.2005.04961.x , PMID 16262702 .