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The allosteric inhibition of glycine transporter 2 by bioactive lipid analgesics is controlled by penetration into a deep lipid cavity.
J Biol Chem. 2021 Jan-Jun;296:100282. doi: 10.1016/j.jbc.2021.100282. Epub 2021 Jan 12.
J Biol Chem. 2021.
PMID: 33450225
Free PMC article.
Synthesis and Characterization of Novel Acyl-Glycine Inhibitors of GlyT2.
Mostyn SN, Carland JE, Shimmon S, Ryan RM, Rawling T, Vandenberg RJ.
Mostyn SN, et al.
ACS Chem Neurosci. 2017 Sep 20;8(9):1949-1959. doi: 10.1021/acschemneuro.7b00105. Epub 2017 Jun 15.
ACS Chem Neurosci. 2017.
PMID: 28574249
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Molecular Determinants for Substrate Interactions with the Glycine Transporter GlyT2.
Carland JE, Thomas M, Mostyn SN, Subramanian N, O'Mara ML, Ryan RM, Vandenberg RJ.
Carland JE, et al. Among authors: mostyn sn.
ACS Chem Neurosci. 2018 Mar 21;9(3):603-614. doi: 10.1021/acschemneuro.7b00407. Epub 2017 Nov 27.
ACS Chem Neurosci. 2018.
PMID: 29120604
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Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain.
Mostyn SN, Rawling T, Mohammadi S, Shimmon S, Frangos ZJ, Sarker S, Yousuf A, Vetter I, Ryan RM, Christie MJ, Vandenberg RJ.
Mostyn SN, et al.
J Med Chem. 2019 Mar 14;62(5):2466-2484. doi: 10.1021/acs.jmedchem.8b01775. Epub 2019 Feb 20.
J Med Chem. 2019.
PMID: 30714733
Free PMC article.
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Identification of an allosteric binding site on the human glycine transporter, GlyT2, for bioactive lipid analgesics.
Mostyn SN, Wilson KA, Schumann-Gillett A, Frangos ZJ, Shimmon S, Rawling T, Ryan RM, O'Mara ML, Vandenberg RJ.
Mostyn SN, et al.
Elife. 2019 Oct 17;8:e47150. doi: 10.7554/eLife.47150.
Elife. 2019.
PMID: 31621581
Free PMC article.
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Photoswitchable ORG25543 Congener Enables Optical Control of Glycine Transporter 2.
Mostyn SN, Sarker S, Muthuraman P, Raja A, Shimmon S, Rawling T, Cioffi CL, Vandenberg RJ.
Mostyn SN, et al.
ACS Chem Neurosci. 2020 May 6;11(9):1250-1258. doi: 10.1021/acschemneuro.9b00655. Epub 2020 Apr 9.
ACS Chem Neurosci. 2020.
PMID: 32191428
Free PMC article.
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Peripheral Administration of Selective Glycine Transporter-2 Inhibitor, Oleoyl-D-Lysine, Reverses Chronic Neuropathic Pain but Not Acute or Inflammatory Pain in Male Mice.
Wilson BS, Peiser-Oliver J, Gillis A, Evans S, Alamein C, Mostyn SN, Shimmon S, Rawling T, Christie MJ, Vandenberg RJ, Mohammadi SA.
Wilson BS, et al. Among authors: mostyn sn.
J Pharmacol Exp Ther. 2022 Sep;382(3):246-255. doi: 10.1124/jpet.122.001265. Epub 2022 Jul 2.
J Pharmacol Exp Ther. 2022.
PMID: 35779948
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Glycine transporter2 inhibitors: Getting the balance right.
Vandenberg RJ, Mostyn SN, Carland JE, Ryan RM.
Vandenberg RJ, et al. Among authors: mostyn sn.
Neurochem Int. 2016 Sep;98:89-93. doi: 10.1016/j.neuint.2015.12.007. Epub 2015 Dec 23.
Neurochem Int. 2016.
PMID: 26723543
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