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AI is a viable alternative to high throughput screening: a 318-target study.
Sci Rep. 2024 Apr 2;14(1):7526. doi: 10.1038/s41598-024-54655-z.
Sci Rep. 2024.
PMID: 38565852
Free PMC article.
The efficacy of the analgesic GlyT2 inhibitor, ORG25543, is determined by two connected allosteric sites.
Chater RC, Quinn AS, Wilson K, Frangos ZJ, Sutton P, Jayakumar S, Cioffi CL, O'Mara ML, Vandenberg RJ.
Chater RC, et al. Among authors: frangos zj.
J Neurochem. 2023 Dec 22. doi: 10.1111/jnc.16028. Online ahead of print.
J Neurochem. 2023.
PMID: 38131125
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Novel Phenylene Lipids That Are Positive Allosteric Modulators of Glycine Receptors and Inhibitors of Glycine Transporter 2.
Gallagher CI, Frangos ZJ, Sheipouri D, Shimmon S, Duman MN, Jayakumar S, Cioffi CL, Rawling T, Vandenberg RJ.
Gallagher CI, et al. Among authors: frangos zj.
ACS Chem Neurosci. 2023 Aug 2;14(15):2634-2647. doi: 10.1021/acschemneuro.3c00167. Epub 2023 Jul 19.
ACS Chem Neurosci. 2023.
PMID: 37466545
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Membrane cholesterol regulates inhibition and substrate transport by the glycine transporter, GlyT2.
Frangos ZJ, Wilson KA, Aitken HM, Cantwell Chater R, Vandenberg RJ, O'Mara ML.
Frangos ZJ, et al.
Life Sci Alliance. 2023 Jan 23;6(4):e202201708. doi: 10.26508/lsa.202201708. Print 2023 Apr.
Life Sci Alliance. 2023.
PMID: 36690444
Free PMC article.
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Glycine Transporter 2: Mechanism and Allosteric Modulation.
Frangos ZJ, Cantwell Chater RP, Vandenberg RJ.
Frangos ZJ, et al.
Front Mol Biosci. 2021 Nov 5;8:734427. doi: 10.3389/fmolb.2021.734427. eCollection 2021.
Front Mol Biosci. 2021.
PMID: 34805268
Free PMC article.
Review.
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The allosteric inhibition of glycine transporter 2 by bioactive lipid analgesics is controlled by penetration into a deep lipid cavity.
Wilson KA, Mostyn SN, Frangos ZJ, Shimmon S, Rawling T, Vandenberg RJ, O'Mara ML.
Wilson KA, et al. Among authors: frangos zj.
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.
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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. Among authors: frangos zj.
Elife. 2019 Oct 17;8:e47150. doi: 10.7554/eLife.47150.
Elife. 2019.
PMID: 31621581
Free PMC article.
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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. Among authors: frangos zj.
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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