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The crystallographic structure of the human adenosine A2A receptor in a high-affinity antagonist-bound state: implications for GPCR drug screening and design.
Jaakola VP, Ijzerman AP. Jaakola VP, et al. Curr Opin Struct Biol. 2010 Aug;20(4):401-14. doi: 10.1016/j.sbi.2010.05.002. Epub 2010 Jun 9. Curr Opin Struct Biol. 2010. PMID: 20538452 Review.
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Chang LC, Spanjersberg RF, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Brussee J, Ijzerman AP. Chang LC, et al. J Med Chem. 2006 May 18;49(10):2861-7. doi: 10.1021/jm050640i. J Med Chem. 2006. PMID: 16686529
Structure-affinity relationships of adenosine A2B receptor ligands.
Beukers MW, Meurs I, Ijzerman AP. Beukers MW, et al. Med Res Rev. 2006 Sep;26(5):667-98. doi: 10.1002/med.20069. Med Res Rev. 2006. PMID: 16847822 Review.
Non-xanthine antagonists for the adenosine A1 receptor.
Chang LC, Brussee J, Ijzerman AP. Chang LC, et al. Chem Biodivers. 2004 Nov;1(11):1591-626. doi: 10.1002/cbdv.200490122. Chem Biodivers. 2004. PMID: 17191804 Review. No abstract available.
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Westerhout J, Spangenberg T, Brussee J, Ijzerman AP. Chang LC, et al. J Med Chem. 2007 Feb 22;50(4):828-34. doi: 10.1021/jm0607956. J Med Chem. 2007. PMID: 17300165
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
van Veldhoven JP, Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Struensee-Link R, Beukers MW, Brussee J, IJzerman AP. van Veldhoven JP, et al. Bioorg Med Chem. 2008 Mar 15;16(6):2741-52. doi: 10.1016/j.bmc.2008.01.013. Epub 2008 Jan 12. Bioorg Med Chem. 2008. PMID: 18258439
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Mantri M, de Graaf O, van Veldhoven J, Göblyös A, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Link R, de Vries H, Beukers MW, Brussee J, Ijzerman AP. Mantri M, et al. J Med Chem. 2008 Aug 14;51(15):4449-55. doi: 10.1021/jm701594y. Epub 2008 Jul 19. J Med Chem. 2008. PMID: 18637670
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.
Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, Ijzerman AP, Stevens RC. Jaakola VP, et al. Science. 2008 Nov 21;322(5905):1211-7. doi: 10.1126/science.1164772. Epub 2008 Oct 2. Science. 2008. PMID: 18832607 Free PMC article.
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists.
Katritch V, Jaakola VP, Lane JR, Lin J, Ijzerman AP, Yeager M, Kufareva I, Stevens RC, Abagyan R. Katritch V, et al. J Med Chem. 2010 Feb 25;53(4):1799-809. doi: 10.1021/jm901647p. J Med Chem. 2010. PMID: 20095623 Free PMC article.
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