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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: veal jm. 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
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. 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
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. Among authors: veal jm. Sci Rep. 2023 Aug 19;13(1):13524. doi: 10.1038/s41598-023-39805-z. Sci Rep. 2023. PMID: 37598239 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. Among authors: veal jm. 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.
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).
Kanouni T, Severin C, Cho RW, Yuen NY, Xu J, Shi L, Lai C, Del Rosario JR, Stansfield RK, Lawton LN, Hosfield D, O'Connell S, Kreilein MM, Tavares-Greco P, Nie Z, Kaldor SW, Veal JM, Stafford JA, Chen YK. Kanouni T, et al. Among authors: veal jm. J Med Chem. 2020 Dec 10;63(23):14522-14529. doi: 10.1021/acs.jmedchem.0c00978. Epub 2020 Oct 9. J Med Chem. 2020. PMID: 33034194
Structure-based design and discovery of potent and selective KDM5 inhibitors.
Nie Z, Shi L, Lai C, O'Connell SM, Xu J, Stansfield RK, Hosfield DJ, Veal JM, Stafford JA. Nie Z, et al. Among authors: veal jm. Bioorg Med Chem Lett. 2018 May 15;28(9):1490-1494. doi: 10.1016/j.bmcl.2018.03.083. Epub 2018 Mar 30. Bioorg Med Chem Lett. 2018. PMID: 29627262
Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models.
Chen YK, Bonaldi T, Cuomo A, Del Rosario JR, Hosfield DJ, Kanouni T, Kao SC, Lai C, Lobo NA, Matuszkiewicz J, McGeehan A, O'Connell SM, Shi L, Stafford JA, Stansfield RK, Veal JM, Weiss MS, Yuen NY, Wallace MB. Chen YK, et al. Among authors: veal jm. ACS Med Chem Lett. 2017 Jul 27;8(8):869-874. doi: 10.1021/acsmedchemlett.7b00220. eCollection 2017 Aug 10. ACS Med Chem Lett. 2017. PMID: 28835804 Free PMC article.
Fluorescence linked enzyme chemoproteomic strategy for discovery of a potent and selective DAPK1 and ZIPK inhibitor.
Carlson DA, Franke AS, Weitzel DH, Speer BL, Hughes PF, Hagerty L, Fortner CN, Veal JM, Barta TE, Zieba BJ, Somlyo AV, Sutherland C, Deng JT, Walsh MP, MacDonald JA, Haystead TA. Carlson DA, et al. Among authors: veal jm. ACS Chem Biol. 2013 Dec 20;8(12):2715-23. doi: 10.1021/cb400407c. Epub 2013 Oct 17. ACS Chem Biol. 2013. PMID: 24070067 Free PMC article.
41 results