Lennart Bunch
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
- 2017
- Published
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, C., Koch, K., Brown, P. M. G. E., Møller, C., Han, L., Huynh, Tri Hien Viet, Hansen, S. W., Nielsen, Birgitte, Bowie, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2017, In: Journal of Medicinal Chemistry. 60, 1, p. 441-457 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2016
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2015
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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, C. S., Hansen, J., Han, L., Monrad, R. N., Nielsen, Birgitte, Tapken, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2015, In: Journal of Medicinal Chemistry. 58, 15, p. 6131-50 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
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
- 2014
- Published
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
- Published
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
- Published
Molecular recognition of two 2,4-syn-functionalized (S)-glutamate analogues by the kainate receptor GluK3 ligand-binding domain
Venskutonyte, R., Larsen, A. P., Frydenvang, Karla Andrea, Gajhede, Michael, Gefflaut, T., Pickering, Darryl S, Bunch, Lennart & Kastrup, Jette Sandholm Jensen, 2014, In: ChemMedChem. 9, 10, p. 2254-2259 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
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
- Published
Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors
Pinto, A., Tamborini, L., Mastronardi, F., Ettari, R., Safoz, Y., Bunch, Lennart, Nielsen, Birgitte, Jensen, Anders A., De Micheli, C. & Conti, P., 2014, In: European Journal of Medicinal Chemistry. 75, p. 151-158 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2013
- Published
Corrigendum to "Binding site and interlobe interactions of the ionotropic glutamate receptor GluK3 ligand binding domain revealed by high resolution crystal structure in complex with (S)-glutamate" [J. Struct. Biol. 176 (2011) 307-314]
Venskutonyte, R., Frydenvang, Karla Andrea, Gajhede, Michael, Bunch, Lennart, Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, Nov 2013, In: Journal of Structural Biology. 184, 2, p. 381 1 p.Research output: Contribution to journal › Comment/debate › Research › peer-review
- Published
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
- Published
Heterocycles as nonclassical bioisosteres of alpha-amino acids
Poulie, Christian Bernard Matthijs & Bunch, Lennart, Feb 2013, In: ChemMedChem. 8, 2, p. 205-215Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
ID: 1302517
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327
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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
Published -
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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19
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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
Published