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Page 1
JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders.
Ambrus-Aikelin G, Takeda K, Joetham A, Lazic M, Povero D, Santini AM, Pranadinata R, Johnson CD, McGeough MD, Beasley FC, Stansfield R, McBride C, Trzoss L, Hoffman HM, Feldstein AE, Stafford JA, Veal JM, Bain G, Gelfand EW. Ambrus-Aikelin G, et al. Sci Rep. 2023 Aug 19;13(1):13524. doi: 10.1038/s41598-023-39805-z. Sci Rep. 2023. PMID: 37598239 Free PMC article.
Pharmacology of a Potent and Novel Inhibitor of the NOD-Like Receptor Pyrin Domain-Containing Protein 3 (NLRP3) Inflammasome that Attenuates Development of Nonalcoholic Steatohepatitis and Liver Fibrosis.
Povero D, Lazic M, McBride C, Ambrus-Aikelin G, Stansfield R, Johnson CD, Santini AM, Pranadinata RF, McGeough MD, Stafford JA, Hoffman HM, Feldstein AE, Veal JM, Bain G. Povero D, et al. Among authors: ambrus aikelin g. J Pharmacol Exp Ther. 2023 Aug;386(2):242-258. doi: 10.1124/jpet.123.001639. Epub 2023 Jun 12. J Pharmacol Exp Ther. 2023. PMID: 37308266
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.
Tanaka Y, Kurasawa O, Yokota A, Klein MG, Ono K, Saito B, Matsumoto S, Okaniwa M, Ambrus-Aikelin G, Morishita D, Kitazawa S, Uchiyama N, Ogawa K, Kimura H, Imamura S. Tanaka Y, et al. Among authors: ambrus aikelin g. J Med Chem. 2020 Mar 26;63(6):3215-3226. doi: 10.1021/acs.jmedchem.9b01979. Epub 2020 Mar 16. J Med Chem. 2020. PMID: 32142284
New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase.
Tanaka Y, Kurasawa O, Yokota A, Klein MG, Saito B, Matsumoto S, Okaniwa M, Ambrus-Aikelin G, Uchiyama N, Morishita D, Kimura H, Imamura S. Tanaka Y, et al. Among authors: ambrus aikelin g. ACS Med Chem Lett. 2020 Jul 30;11(8):1645-1652. doi: 10.1021/acsmedchemlett.0c00331. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 34345355 Free PMC article.
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
McBride C, Trzoss L, Povero D, Lazic M, Ambrus-Aikelin G, Santini A, Pranadinata R, Bain G, Stansfield R, Stafford JA, Veal J, Takahashi R, Ly J, Chen S, Liu L, Nespi M, Blake R, Katewa A, Kleinheinz T, Sujatha-Bhaskar S, Ramamoorthi N, Sims J, McKenzie B, Chen M, Ultsch M, Johnson M, Murray J, Ciferri C, Staben ST, Townsend MJ, Stivala CE. McBride C, et al. Among authors: ambrus aikelin g. J Med Chem. 2022 Nov 10;65(21):14721-14739. doi: 10.1021/acs.jmedchem.2c01250. Epub 2022 Oct 24. J Med Chem. 2022. PMID: 36279149
Cholesterol Unbound RORγt Protein Enables a Sensitive Inverse Agonist Screening.
Koyama R, Fukuda Y, Kamada Y, Nakagawa H, Witmer D, Ambrus-Aikelin G, Sang BC, Nakayama M, Iwata H. Koyama R, et al. Among authors: ambrus aikelin g. Assay Drug Dev Technol. 2018 May/Jun;16(4):194-204. doi: 10.1089/adt.2018.852. Epub 2018 Jun 6. Assay Drug Dev Technol. 2018. PMID: 29874096
Early pathways, biomarkers, and four distinct molecular subclasses of preeclampsia: The intersection of clinical, pathological, and high-dimensional biology studies.
Than NG, Posta M, Györffy D, Orosz L, Orosz G, Rossi SW, Ambrus-Aikelin G, Szilágyi A, Nagy S, Hupuczi P, Török O, Tarca AL, Erez O, Papp Z, Romero R. Than NG, et al. Among authors: ambrus aikelin g. Placenta. 2022 Jul;125:10-19. doi: 10.1016/j.placenta.2022.03.009. Epub 2022 Mar 22. Placenta. 2022. PMID: 35428514 Free PMC article.
Author Correction: JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders.
Ambrus-Aikelin G, Takeda K, Joetham A, Lazic M, Povero D, Santini AM, Pranadinata R, Johnson CD, McGeough MD, Beasley FC, Stansfield R, McBride C, Trzoss L, Hoffman HM, Feldstein AE, Stafford JA, Veal JM, Bain G, Gelfand EW. Ambrus-Aikelin G, et al. Sci Rep. 2023 Nov 16;13(1):20081. doi: 10.1038/s41598-023-47251-0. Sci Rep. 2023. PMID: 37973811 Free PMC article. No abstract available.