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Inhibitors of histone demethylases.
Lohse B, Kristensen JL, Kristensen LH, Agger K, Helin K, Gajhede M, Clausen RP. Lohse B, et al. Among authors: gajhede m. Bioorg Med Chem. 2011 Jun 15;19(12):3625-36. doi: 10.1016/j.bmc.2011.01.046. Epub 2011 Feb 1. Bioorg Med Chem. 2011. PMID: 21596573 Review.
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
Vogensen SB, Frydenvang K, Greenwood JR, Postorino G, Nielsen B, Pickering DS, Ebert B, Bølcho U, Egebjerg J, Gajhede M, Kastrup JS, Johansen TN, Clausen RP, Krogsgaard-Larsen P. Vogensen SB, et al. Among authors: gajhede m. J Med Chem. 2007 May 17;50(10):2408-14. doi: 10.1021/jm061439q. Epub 2007 Apr 25. J Med Chem. 2007. PMID: 17455929
Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.
Beich-Frandsen M, Pickering DS, Mirza O, Johansen TN, Greenwood J, Vestergaard B, Schousboe A, Gajhede M, Liljefors T, Kastrup JS. Beich-Frandsen M, et al. Among authors: gajhede m. J Med Chem. 2008 Mar 13;51(5):1459-63. doi: 10.1021/jm701126w. Epub 2008 Feb 13. J Med Chem. 2008. PMID: 18269227
Full domain closure of the ligand-binding core of the ionotropic glutamate receptor iGluR5 induced by the high affinity agonist dysiherbaine and the functional antagonist 8,9-dideoxyneodysiherbaine.
Frydenvang K, Lash LL, Naur P, Postila PA, Pickering DS, Smith CM, Gajhede M, Sasaki M, Sakai R, Pentikaïnen OT, Swanson GT, Kastrup JS. Frydenvang K, et al. Among authors: gajhede m. J Biol Chem. 2009 May 22;284(21):14219-29. doi: 10.1074/jbc.M808547200. Epub 2009 Mar 18. J Biol Chem. 2009. PMID: 19297335 Free PMC article.
The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.
Clausen RP, Naur P, Kristensen AS, Greenwood JR, Strange M, Bräuner-Osborne H, Jensen AA, Nielsen AS, Geneser U, Ringgaard LM, Nielsen B, Pickering DS, Brehm L, Gajhede M, Krogsgaard-Larsen P, Kastrup JS. Clausen RP, et al. Among authors: gajhede m. J Med Chem. 2009 Aug 13;52(15):4911-22. doi: 10.1021/jm900565c. J Med Chem. 2009. PMID: 19588945
Enzyme kinetic studies of histone demethylases KDM4C and KDM6A: towards understanding selectivity of inhibitors targeting oncogenic histone demethylases.
Kristensen JB, Nielsen AL, Jørgensen L, Kristensen LH, Helgstrand C, Juknaite L, Kristensen JL, Kastrup JS, Clausen RP, Olsen L, Gajhede M. Kristensen JB, et al. Among authors: gajhede m. FEBS Lett. 2011 Jun 23;585(12):1951-6. doi: 10.1016/j.febslet.2011.05.023. Epub 2011 May 12. FEBS Lett. 2011. PMID: 21575637 Free article.
Studies of H3K4me3 demethylation by KDM5B/Jarid1B/PLU1 reveals strong substrate recognition in vitro and identifies 2,4-pyridine-dicarboxylic acid as an in vitro and in cell inhibitor.
Kristensen LH, Nielsen AL, Helgstrand C, Lees M, Cloos P, Kastrup JS, Helin K, Olsen L, Gajhede M. Kristensen LH, et al. Among authors: gajhede m. FEBS J. 2012 Jun;279(11):1905-14. doi: 10.1111/j.1742-4658.2012.08567.x. Epub 2012 May 2. FEBS J. 2012. PMID: 22420752 Free article.
Identification of catechols as histone-lysine demethylase inhibitors.
Nielsen AL, Kristensen LH, Stephansen KB, Kristensen JB, Helgstrand C, Lees M, Cloos P, Helin K, Gajhede M, Olsen L. Nielsen AL, et al. Among authors: gajhede m. FEBS Lett. 2012 Apr 24;586(8):1190-4. doi: 10.1016/j.febslet.2012.03.001. Epub 2012 Mar 15. FEBS Lett. 2012. PMID: 22575654 Free article.
144 results