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Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity.
Borodovsky A, Barbon CM, Wang Y, Ye M, Prickett L, Chandra D, Shaw J, Deng N, Sachsenmeier K, Clarke JD, Linghu B, Brown GA, Brown J, Congreve M, Cheng RK, Dore AS, Hurrell E, Shao W, Woessner R, Reimer C, Drew L, Fawell S, Schuller AG, Mele DA. Borodovsky A, et al. Among authors: congreve m. J Immunother Cancer. 2020 Jul;8(2):e000417. doi: 10.1136/jitc-2019-000417. J Immunother Cancer. 2020. PMID: 32727810 Free PMC article.
Identification of novel adenosine A(2A) receptor antagonists by virtual screening.
Langmead CJ, Andrews SP, Congreve M, Errey JC, Hurrell E, Marshall FH, Mason JS, Richardson CM, Robertson N, Zhukov A, Weir M. Langmead CJ, et al. Among authors: congreve m. J Med Chem. 2012 Mar 8;55(5):1904-9. doi: 10.1021/jm201455y. Epub 2012 Feb 23. J Med Chem. 2012. PMID: 22250781 Free PMC article.
Intracellular allosteric antagonism of the CCR9 receptor.
Oswald C, Rappas M, Kean J, Doré AS, Errey JC, Bennett K, Deflorian F, Christopher JA, Jazayeri A, Mason JS, Congreve M, Cooke RM, Marshall FH. Oswald C, et al. Among authors: congreve m. Nature. 2016 Dec 15;540(7633):462-465. doi: 10.1038/nature20606. Epub 2016 Dec 7. Nature. 2016. PMID: 27926729
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. Christopher JA, et al. Among authors: congreve m. J Med Chem. 2015 Aug 27;58(16):6653-64. doi: 10.1021/acs.jmedchem.5b00892. Epub 2015 Aug 12. J Med Chem. 2015. PMID: 26225459
X-Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists.
Jespers W, Verdon G, Azuaje J, Majellaro M, Keränen H, García-Mera X, Congreve M, Deflorian F, de Graaf C, Zhukov A, Doré AS, Mason JS, Åqvist J, Cooke RM, Sotelo E, Gutiérrez-de-Terán H. Jespers W, et al. Among authors: congreve m. Angew Chem Int Ed Engl. 2020 Sep 14;59(38):16536-16543. doi: 10.1002/anie.202003788. Epub 2020 Jul 22. Angew Chem Int Ed Engl. 2020. PMID: 32542862 Free PMC article.
73 results