Biology:Vesicular acetylcholine transporter
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Short description: Protein-coding gene in the species Homo sapiens
 Generic protein structure example |
The Vesicular acetylcholine transporter (VAChT) is a neurotransmitter transporter which is responsible for loading acetylcholine (ACh) into secretory organelles in neurons making acetylcholine available for secretion.[1][2] It is encoded by Solute carrier family 18, member 3 (SLC18A3) gene, located within the first intron of the choline acetyltransferase gene. VAChT is able to transport ACh into vesicles by relying on an exchange between protons (H+) that were previously pumped into the vesicle diffusing out, thus acting as an antiporter. ACh molecules are then carried into the vesicle by the action of exiting protons.[3] Acetylcholine transport utilizes a proton gradient established by a vacuolar ATPase.
VAChT uptake inhibitors
Radiolabeled compounds
PET imaging of the VAChT may provide insights into early diagnosis of Alzheimer's disease.
- (−)-trans-2-Hydroxy-3-(4-(4-[18F]fluorobenzoyl)piperidino)tetralin; racemate: Ki = 2.70 nM for VAChT, 191 nM for σ1, and 251 nM for σ2[4]
References
- ↑ "Molecular analysis of vesicular amine transporter function and targeting to secretory organelles". FASEB Journal 14 (15): 2450–8. Dec 2000. doi:10.1096/fj.00-0206rev. PMID 11099462.
- ↑ "Visualization of the vesicular acetylcholine transporter in cholinergic nerve terminals and its targeting to a specific population of small synaptic vesicles". Proceedings of the National Academy of Sciences of the United States of America 93 (8): 3547–52. Apr 1996. doi:10.1073/pnas.93.8.3547. PMID 8622973.
- ↑ Waymire, Jack. "Storage of ACh". University of Texas Medical Center. http://neuroscience.uth.tmc.edu/s1/chapter11.html.
- ↑ "Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter". Journal of Medicinal Chemistry 52 (5): 1358–69. Mar 2009. doi:10.1021/jm8012344. PMID 19203271.
Further reading
- "Nuclear choline acetyltransferase activates transcription of a high-affinity choline transporter". The Journal of Biological Chemistry 286 (7): 5836–45. Feb 2011. doi:10.1074/jbc.M110.147611. PMID 21163949.
- "Inhibition of cholinergic signaling causes apoptosis in human bronchioalveolar carcinoma". Cancer Research 73 (4): 1328–39. Feb 2013. doi:10.1158/0008-5472.CAN-12-3190. PMID 23222296. PMC 10461321. https://works.bepress.com/jamie_lau/3/download/.
- "Active transport of acetylcholine by the human vesicular acetylcholine transporter". The Journal of Biological Chemistry 271 (44): 27229–32. Nov 1996. doi:10.1074/jbc.271.44.27229. PMID 8910293.
- "Sequence variation in the CHAT locus shows no association with late-onset Alzheimer's disease". Human Genetics 113 (3): 258–67. Aug 2003. doi:10.1007/s00439-003-0960-2. PMID 12759818.
- "Association studies of 23 positional/functional candidate genes on chromosome 10 in late-onset Alzheimer's disease". American Journal of Medical Genetics Part B 144B (6): 762–70. Sep 2007. doi:10.1002/ajmg.b.30509. PMID 17373700.
- "Somatomotor neuron-specific expression of the human cholinergic gene locus in transgenic mice". Neuroscience 96 (4): 707–22. 2000. doi:10.1016/s0306-4522(99)00587-4. PMID 10727789.
- "Search for the acetylcholine and vesamicol binding sites in vesicular acetylcholine transporter: the region around the lumenal end of the transport channel". Journal of Neurochemistry 115 (4): 984–93. Nov 2010. doi:10.1111/j.1471-4159.2010.06990.x. PMID 20831599.
- "Immunochemical and immunocytochemical characterization of cholinergic markers in human peripheral blood lymphocytes". Journal of Neuroimmunology 132 (1–2): 147–55. Nov 2002. doi:10.1016/s0165-5728(02)00325-9. PMID 12417445.
- "Human choline acetyltransferase gene: localization of alternative first exons". Journal of Neuroscience Research 40 (4): 427–38. Mar 1995. doi:10.1002/jnr.490400402. PMID 7616604.
External links
- Vesicular+Acetylcholine+Transporter at the US National Library of Medicine Medical Subject Headings (MeSH)
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