Lennart Bunch
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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Allosteric modulation of an excitatory amino acid transporter: The subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain
Abrahamsen, B., Schneider, N., Erichsen, M. N., Huynh, Tri Hien Viet, Fahlke, C., Bunch, Lennart & Jensen, Anders A., 2013, In: Journal of Neuroscience. 33, 3, p. 1068-1087Research output: Contribution to journal › Journal article › Research › peer-review
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Chemoenzymatic synthesis of a series of 4-substituted glutamate analogues and pharmacological characterization at human glutamate transporters subtypes 1-3
Alaux, S., Kusk, M., Sagot, E., Bolte, J., Jensen, Anders A., Bräuner, Hans, Gefflaut, T. & Bunch, Lennart, 2005, In: Journal of Medicinal Chemistry. 48, 25, p. 7980-92 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)
Alcaide, A., Marconi, L., Marek, A., Haym, I., Nielsen, Birgitte, Møllerud, S., Jensen, M., Conti, P., Pickering, Darryl S & Bunch, Lennart, 2016, In: MedChemComm. 7, p. 2136-2144 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Chemo-enzymatic 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, A. P., Venskutonyte, R., Han, L., Abrahamsen, B., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Jensen, Anders A., Pickering, Darryl S, Frydenvang, Karla Andrea, Gefflaut, T. & Bunch, Lennart, 2013, In: Journal of Medicinal Chemistry. 56, 4, p. 1614-1628Research output: Contribution to journal › Journal article › Research › peer-review
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Erratum: 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 (Journal of Medicinal Chemistry (2013) 56 (1614-1628))
Assaf, Z., Larsen, A. P., Venskutonyteì, R., Han, L., Abrahamsen, B., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Jensen, A. A., Pickering, Darryl S, Frydenvang, Karla Andrea, Gefflaut, T. & Bunch, Lennart, 25 Jul 2013, In: Journal of Medicinal Chemistry. 56, 14, p. 5985 1 p.Research output: Contribution to journal › Comment/debate › Research › peer-review
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In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs
Bechthold, E., Grey, L., Diamant, E., Schmidt, J., Steigerwald, R., Zhao, F., Hansen, K. B., Bunch, Lennart, Clausen, Rasmus Prætorius & Wünsch, B., 2023, In: Biological Chemistry. 404, 4, p. 255-265Research output: Contribution to journal › Journal article › Research › peer-review
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Functionalization of Oxazolo[4,5-b]pyrazines by Deprotometallation
Bisballe, N., Hedidi, M., Demmer, C. S., Chevallier, F., Roisnel, T., Dorcet, V., Halauko, Y. S., Ivashkevich, O. A., Matulis, V. E., Bentabed-Ababsa, G., Bunch, Lennart & Mongin, F., 7 Aug 2018, In: European Journal of Organic Chemistry. 29, p. 3904-3913Research output: Contribution to journal › Journal article › Research › peer-review
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Azetidinic amino acids: stereocontrolled synthesis and pharmacological characterization as ligands for glutamate receptors and transporters
Bräuner, Hans, Bunch, Lennart, Chopin, N., Couty, F., Evano, G., Jensen, Anders A., Kusk, M. L., Nielsen, Birgitte & Rabasso, N., 2005, In: Organic & Biomolecular Chemistry. 3, 21, p. 3926-36 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Unprecedented migration of N-alkoxycarbonyl groups in protected pyroglutaminol
Bunch, Lennart, Norrby, P., Frydenvang, Karla Andrea, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2001, In: Organic Letters. 3, 3, p. 433-5 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and receptor binding affinity of new selective GluR5 ligands
Bunch, Lennart, Johansen, T. H., Bräuner, Hans, Stensbøl, T. B., Johansen, Tommy Nørskov, Krogsgaard-Larsen, Povl & Madsen, Ulf, Apr 2001, In: Bioorganic & Medicinal Chemistry. 9, 4, p. 875-9Research output: Contribution to journal › Journal article › Research › peer-review
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Subtype selective kainic acid receptor agonists: discovery and approaches to rational design
Bunch, Lennart & Krogsgaard-Larsen, Povl, 2009, In: Medicinal Research Reviews. 29, 1, p. 3-28Research output: Contribution to journal › Review › Research › peer-review
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Mixed cyano-gilman cuprates - Advances in conjugate addition to alpha,beta-unsaturated pyroglutaminol
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, Jan 2002, In: Synthesis. 1, p. 31-33Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid transporters as potential drug targets
Bunch, Lennart, Erichsen, M. N. & Jensen, Anders A., 2009, In: Expert Opinion On Therapeutic Targets. 13, 6, p. 719-731Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design and enantioselective synthesis of (1R,4S,5R,6S)-3-azabicyclo[3.3.0]octane-4,6-dicarboxylic acid - a novel inhibitor at human glutamate transporter subtypes 1, 2, and 3
Bunch, Lennart, Nielsen, Birgitte, Jensen, Anders A. & Bräuner, Hans, 2006, In: Journal of Medicinal Chemistry. 49, 1, p. 172-8 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters
Bunch, Lennart, Pickering, Darryl S, Gefflaut, T., Vinatier, V., Helaine, V., Amir, A., Nielsen, Birgitte & Jensen, Anders A., 2009, In: ChemMedChem. 4, 11, p. 1925-1929Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors: focus on subtypes iGlu5-7
Bunch, Lennart, Gefflaut, T., Alaux, S., Sagot, E., Nielsen, Birgitte & Pickering, Darryl S, 2009, In: European Journal of Pharmacology. 609, p. 1-4Research output: Contribution to journal › Journal article › Research › peer-review
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Regioselective lithiation and functionalization of 3-(benzyloxy)isothiazole: Application to the synthesis of thioibotenic acid
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, 5 Apr 2002, In: Journal of Organic Chemistry. 67, 7, p. 2375-2377Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design, synthesis, and pharmacological evaluation of 2-azanorbornane-3-exo,5-endo-dicarboxylic acid: a novel conformationally restricted glutamic acid analogue
Bunch, Lennart, Liljefors, T., Greenwood, J. R., Frydenvang, Karla Andrea, Bräuner, Hans, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2003, In: Journal of Organic Chemistry. 68, 4, p. 1489-95 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Physiology, pharmacology and pathophysiology of the pH regulatory transport proteins NHE1 and NBCn1: similarities, differences, and implications for cancer therapy
Bødtkjer, E., Bunch, Lennart & Pedersen, Stine Helene Falsig, 2012, In: Current Pharmaceutical Design. 18, 10, p. 1345-1371 27 p.Research output: Contribution to journal › Journal article › Research › peer-review
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The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
Cuesta, E. P., Christensen, S., Jensen, Anders A., Jensen, N. F., Bunch, Lennart, Rømer, M. U. K., Brünner, N., Stenvang, Jan & Pedersen, Stine Helene Falsig, 2015, In: B M C Cancer. 15, 1, 17 p., 411.Research output: Contribution to journal › Journal article › Research › peer-review
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Binding Mode of an α-Amino Acid-Linked Quinoxaline-2,3-dione Analogue at Glutamate Receptor Subtype GluK1
Demmer, C. S., Møller, C., Brown, P. M. G. E., Han, L., Pickering, Darryl S, Nielsen, Birgitte, Bowie, D., Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen & Bunch, Lennart, 9 Apr 2015, In: A C S Chemical Neuroscience. 6, p. 845-854 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Review on modern advances of chemical methods for the introduction of a phosphonic acid group
Demmer, C. S., Krogsgaard-Larsen, N. & Bunch, Lennart, 2011, In: Chemical Reviews. 111, 12, p. 7981-8006Research output: Contribution to journal › Review › Research › peer-review
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Benzoxazoles and oxazolopyridines in medicinal chemistry studies
Demmer, C. S. & Bunch, Lennart, 2015, In: European Journal of Medicinal Chemistry. 97, p. 778-785 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Study of Oxidative Cyclization Using PhI(OAc)(2) in the Formation of Benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles and Related Heterocycles - Scope and Limitations
Demmer, C. S., Jorgensen, M., Kehler, J. & Bunch, Lennart, Jun 2014, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 25, 9, p. 1279-1282 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New Palladium-Catalyzed Domino Reaction with Intramolecular Ring Closure of an N-(2-Chloro-3-heteroaryl) arylamide: First Synthesis of Oxazolo[4,5-b] pyrazines
Demmer, C. S., Hansen, J. C., Kehler, J. & Bunch, Lennart, 24 Mar 2014, In: Advanced Synthesis & Catalysis. 356, 5, p. 1047-1055 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and Selective Functionalization of [1,2,4]Triazolo[4,3-a]pyrazines
Demmer, C. S., Jorgensen, M., Kehler, J., Bunch, Lennart & Rasmussen, L. K., 2015, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 26, 4, p. 519-524 6 p.Research output: Contribution to journal › Letter › Research › peer-review
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Revisiting the Quinoxalinedione scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors.
Demmer, C. S., Rombach, D., Liu, N., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 1 Dec 2017, In: A C S Chemical Neuroscience. 8, 11, p. 2477-2495 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Probing for improved potency and in vivo bioavailability of excitatory amino acid transporter subtype 1 inhibitors UCPH-101 and UCPH-102: Design, synthesis and pharmacological evaluation of substituted 7-biphenyl analogs
Erichsen, M. N., Hansen, J., Artacho Ruiz, J., Demmer, C. S., Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Jensen, Anders A. & Bunch, Lennart, 2014, In: Neurochemical Research. 39, 10, p. 1964-1979 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)
Erichsen, M. N., Huynh, Tri Hien Viet, Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Monrad, O., Bekker-Jensen, A., Nielsen, C. W., Frydenvang, Karla Andrea, Jensen, Anders A. & Bunch, Lennart, 2010, In: Journal of Medicinal Chemistry. 53, 19, p. 7180–7191Research output: Contribution to journal › Journal article › Research › peer-review
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Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3
Faure, S., Jensen, Anders A., Maurat, V., Gu, X., Sagot, E., Aitken, D. J., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2006, In: Journal of Medicinal Chemistry. 49, 22, p. 6532-8 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors
Fu, H., Zhang, J., Tepper, P. G., Bunch, Lennart, Jensen, Anders A. & Poelarends, G. J., 13 Sep 2018, In: Journal of Medicinal Chemistry. 61, 17, p. 7741-7753Research output: Contribution to journal › Journal article › Research › peer-review
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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, J. C., Hansen, K. B., Malm, T., Ishchenko, Y., Larsen, Y., Han, L., Kayser, S., Auriola, S., Petsalo, A., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 14 Dec 2017, In: Journal of Medicinal Chemistry. 60, 23, p. 9885-9904 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Blood-brain barrier permeability and brain uptake mechanism of kainic Acid and dihydrokainic Acid
Gynther, M., Petsalo, A., Hansen, S. H., Bunch, Lennart & Pickering, Darryl S, Mar 2015, In: Neurochemical Research. 40, 3, p. 542-549 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A multifaceted GABAA receptor modulator: Functional properties and mechanism of action of the sedative-hypnotic and recreational drug methaqualone (Quaalude)
Hammer, H., Bader, B. M., Ehnert, C., Bundgaard, C., Bunch, Lennart, Hoestgaard-Jensen, K., Schroeder, O. H., Bastlund, J. F., Gramowski-Voß, A. & Jensen, Anders A., 2015, In: Molecular Pharmacology. 88, 2, p. 401-420 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Convenient access to β-substituted cysteines and β- and γ-mercapto prolines
Hansen, J. C., Rabuffetti, M. & Bunch, Lennart, 2023, In: Canadian Journal of Chemistry. 101, 5, p. 326-333Research output: Contribution to journal › Journal article › Research › peer-review
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Beta-Sulfonamido Functionalized Aspartate Analogs as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype-Selectivity Profiles Arising from Subtle Structural Differences
Hansen, J. C., Bjørn-Yoshimoto, Walden, Bisballe, N., Nielsen, Birgitte, Jensen, Anders A. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, p. 8771-8786 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New insights into the structure-activity-relationship of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitors UCPH-101 and UCPH-102
Hansen, S. W., Erichsen, M. N., Huynh, Tri Hien Viet, Ruiz, J. A., Haym, I., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Hansen, Jeanette Venla, Storgaard, M., Eriksen, A. L., Jensen, Anders A. & Bunch, Lennart, 2016, In: ChemMedChem. 11, 4, p. 382-402 21 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity-Relationship Study
Hansen, S. W., Erichsen, M. N., Fu, B., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Hansen, J. C., Jensen, Anders A. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, 19, p. 8757-8770 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Semi-synthesis of novel buprenorphine derivatives and their anti-nociceptive properties and dependency potential
Hasanpour, Z., Salehi, P., Bunch, Lennart, Khoramjouy, M., Bararjanian, M., Stærk, Dan & Faizi, M., 2021, In: Canadian Journal of Chemistry. 99, 11, p. 910-919Research output: Contribution to journal › Journal article › Research › peer-review
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Bioavailability studies and in vitro profiling of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-102)
Haym, I., Huynh, Tri Hien Viet, Hansen, S. W., Pedersen, M. H. F., Ruiz, J. A., Erichsen, M. N., Gynther, M., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Eriksen, A. L., Jensen, Anders A. & Bunch, Lennart, 2016, In: ChemMedChem. 11, 4, p. 403-419 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Ibotenic acid and thioibotenic acid: a remarkable difference in activity at group III metabotropic glutamate receptors
Hermit, M. B., Greenwood, J. R., Nielsen, Birgitte, Bunch, Lennart, Jørgensen, Charlotte Grube, Vestergaard, H. T., Stensbøl, T. B., Sanchez, C., Krogsgaard-Larsen, Povl, Madsen, Ulf & Bräuner, Hans, 23 Feb 2004, In: European Journal of Pharmacology. 486, 3, p. 241-50Research output: Contribution to journal › Journal article › Research › peer-review
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Profiling substrate specificity of two series of phenethylamine analogs at monoamine oxidase A and B
Heuson, E., Storgaard, M., Huynh, Tri Hien Viet, Charmantray, F., Gefflaut, T. & Bunch, Lennart, 2014, In: Organic & Biomolecular Chemistry. 12, 43, p. 8689-8695 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configurational assignment using infrared and vibrational circular dichroism spectroscopy in combination with ab initio hartree-fock calculations
Huynh, Tri Hien Viet, Shim, I., Bohr, H., Abrahamsen, B., Nielsen, Birgitte, Jensen, Anders A. & Bunch, Lennart, 2012, In: Journal of Medicinal Chemistry. 55, 11, p. 5403-12 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III
Huynh, Tri Hien Viet, Erichsen, M. N., Tora, A. S., Goudet, C., Sagot, E., Assaf, Z., Thomsen, C., Brodbeck, R., Stensbol, T. B., Bjørn-Yoshimoto, Walden, Nielsen, Birgitte, Pin, J., Gefflaut, T. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, 3, p. 914-924 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the excitatory amino acid transporters (EAATs): Improving the potency of a micromolar screening hit is not truism
Huynh, Tri Hien Viet, Demmer, C. S., Abrahamsen, B., Marcher, Emil, Frykman, M., Jensen, Anders A. & Bunch, Lennart, 2013, In: SpringerPlus. 2, p. 112Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102
Huynh, Tri Hien Viet, Abrahamsen, B., Madsen, K. K., Gonzalez-Franquesa, A., Jensen, Anders A. & Bunch, Lennart, 2012, In: Bioorganic & Medicinal Chemistry. 20, 23, p. 6831-6839Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid transporters: recent insights into molecular mechanisms, novel modes of modulation and new therapeutic possibilities
Jensen, Anders A., Fahlke, C., Bjørn-Yoshimoto, Walden & Bunch, Lennart, 2015, In: Current Opinion in Pharmacology. 20, p. 116-123 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
Jensen, Anders A., Erichsen, M. N., Nielsen, C. W., Stensbøl, T. B., Kehler, J. & Bunch, Lennart, 2009, In: Journal of Medicinal Chemistry. 52, 4, p. 912-915Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors
Juknaite, L., Venskutonyte, R., Assaf, Z., Faure, S., Gefflaut, T., Aitken, D. J., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Bunch, Lennart, Frydenvang, Karla Andrea & Pickering, Darryl S, 2012, In: Journal of Structural Biology. 180, 1, p. 39-46Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302517
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The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
Research output: Contribution to journal › Journal article › Research › peer-review
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195
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Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors
Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of phenol derivatives from cyclopentenones with arynes as key intermediates
Research output: Contribution to journal › Journal article › Research › peer-review
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