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( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
Brogi S, Brindisi M, Butini S, Kshirsagar GU, Maramai S, Chemi G, Gemma S, Campiani G, Novellino E, Fiorenzani P, Pinassi J, Aloisi AM, Gynther M, Venskutonytė R, Han L, Frydenvang K, Kastrup JS, Pickering DS. Brogi S, et al. Among authors: han l. J Med Chem. 2018 Mar 8;61(5):2124-2130. doi: 10.1021/acs.jmedchem.8b00099. Epub 2018 Feb 26. J Med Chem. 2018. PMID: 29451794
Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.
Assaf Z, Larsen AP, Venskutonytė R, Han L, Abrahamsen B, Nielsen B, Gajhede M, Kastrup JS, Jensen AA, Pickering DS, Frydenvang K, Gefflaut T, Bunch L. Assaf Z, et al. Among authors: han l. J Med Chem. 2013 Feb 28;56(4):1614-28. doi: 10.1021/jm301433m. Epub 2013 Feb 15. J Med Chem. 2013. PMID: 23414088
Design, synthesis and in vitro pharmacology of GluK1 and GluK3 antagonists. Studies towards the design of subtype-selective antagonists through 2-carboxyethyl-phenylalanines with substituents interacting with non-conserved residues in the GluK binding sites.
Sköld N, Nielsen B, Olsen J, Han L, Olsen L, Madsen U, Kristensen JL, Pickering DS, Johansen TN. Sköld N, et al. Among authors: han l. Bioorg Med Chem. 2014 Oct 1;22(19):5368-77. doi: 10.1016/j.bmc.2014.07.045. Epub 2014 Aug 2. Bioorg Med Chem. 2014. PMID: 25172149
Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.
Krogsgaard-Larsen N, Storgaard M, Møller C, Demmer CS, Hansen J, Han L, Monrad RN, Nielsen B, Tapken D, Pickering DS, Kastrup JS, Frydenvang K, Bunch L. Krogsgaard-Larsen N, et al. Among authors: han l. J Med Chem. 2015 Aug 13;58(15):6131-50. doi: 10.1021/acs.jmedchem.5b00750. Epub 2015 Jul 22. J Med Chem. 2015. PMID: 26200741
N1-Substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists: X-ray Crystallography, Structure-Affinity Relationships, and in Vitro Pharmacology.
Pallesen J, Møllerud S, Frydenvang K, Pickering DS, Bornholdt J, Nielsen B, Pasini D, Han L, Marconi L, Kastrup JS, Johansen TN. Pallesen J, et al. Among authors: han l. ACS Chem Neurosci. 2019 Mar 20;10(3):1841-1853. doi: 10.1021/acschemneuro.8b00726. Epub 2019 Jan 23. ACS Chem Neurosci. 2019. PMID: 30620174
Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid.
Krogsgaard-Larsen N, Delgar CG, Koch K, Brown PM, Møller C, Han L, Huynh TH, Hansen SW, Nielsen B, Bowie D, Pickering DS, Kastrup JS, Frydenvang K, Bunch L. Krogsgaard-Larsen N, et al. Among authors: han l. J Med Chem. 2017 Jan 12;60(1):441-457. doi: 10.1021/acs.jmedchem.6b01516. Epub 2016 Dec 22. J Med Chem. 2017. PMID: 28005385
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
Gynther M, Proietti Silvestri I, Hansen JC, Hansen KB, Malm T, Ishchenko Y, Larsen Y, Han L, Kayser S, Auriola S, Petsalo A, Nielsen B, Pickering DS, Bunch L. Gynther M, et al. Among authors: han l. J Med Chem. 2017 Dec 14;60(23):9885-9904. doi: 10.1021/acs.jmedchem.7b01624. Epub 2017 Dec 5. J Med Chem. 2017. PMID: 29205034 Free PMC article.
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