ABHD12

alpha/beta-Hydrolase domain containing 12 (ABHD12) is a serine hydrolase encoded by the ABHD12 gene that participates in the breakdown of the endocannabinoid neurotransmitter 2-arachidonylglycerol (2-AG) in the central nervous system.[1] It is responsible for about 9% of brain 2-AG hydrolysis.[1] Together, ABHD12 along with two other enzymes, monoacylglycerol lipase (MAGL) and ABHD6, control 99% of 2-AG hydrolysis in the brain.[1][2] ABHD12 also serves as a lysophospholipase and metabolizes lysophosphatidylserine (LPS).[3]

Inhibitors

Inhibitors of ABHD12 have been identified.[3] Orlistat (tetrahydrolipstatin; THL) and methyl arachidonyl fluorophosphonate (MAFP), so-called "universal lipase/serine hydrolase inhibitors" that are extremely non-selective enzyme inhibitors, were found to inhibit ABHD12.[3] Selective reversible inhibitors have also been identified, including betulinic acid, maslinic acid, oleanolic acid, and ursolic acid.[3]

See also

References

  1. 1 2 3 Cannabinoid Receptors—Advances in Research and Application: 2012 Edition: ScholarlyBrief. ScholarlyEditions. 26 December 2012. pp. 68–. ISBN 978-1-4816-0672-1.
  2. ↑ Savinainen JR, Saario SM, Laitinen JT (February 2012). "The serine hydrolases MAGL, ABHD6 and ABHD12 as guardians of 2-arachidonoylglycerol signalling through cannabinoid receptors". Acta Physiol (Oxf). 204 (2): 267–76. doi:10.1111/j.1748-1716.2011.02280.x. PMC 3320662Freely accessible. PMID 21418147.
  3. 1 2 3 4 Bogyo, Matthew; Parkkari, Teija; Haavikko, Raisa; Laitinen, Tuomo; Navia-Paldanius, Dina; Rytilahti, Roosa; Vaara, Miia; Lehtonen, Marko; Alakurtti, Sami; Yli-Kauhaluoma, Jari; Nevalainen, Tapio; Savinainen, Juha R.; Laitinen, Jarmo T. (2014). "Discovery of Triterpenoids as Reversible Inhibitors of α/β-hydrolase Domain Containing 12 (ABHD12)". PLoS ONE. 9 (5): e98286. doi:10.1371/journal.pone.0098286. ISSN 1932-6203.


This article is issued from Wikipedia - version of the 10/23/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.