Bente Frølund
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
- 2023
- Published
CaMK2 modulators and their use in medicine
Frølund, Bente, Shehata, M. A., Wellendorph, Petrine, Gauger, Stine Juul, Kuriyan, J., McSpadden, E. D., Poulsen, Lasse Brokmose, Fougiaxis, V. & Daraj, K., 2023, IPC No. A61K31/4164, A61K31/4178, A61P25/00, C07D277/06, C07D277/12, C07D277/56, C07D417/04, C07D417/10, Patent No. WO2023170024A1, 1 Jan 1970, Priority No. US202263318852PResearch output: Patent
- Published
Muscimol inhibits plasma membrane rupture and ninjurin-1 oligomerization during pyroptosis
den Hartigh, A. B., Loomis, W. P., Anderson, M. J., Frølund, Bente & Fink, S. L., 2023, In: Communications Biology . 6, 1, 1010.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Pregnenolone sulfate analogues differentially modulate GABAA receptor closed/desensitised states
Mortensen, M., Xu, Y., Shehata, M. A., Krall, J., Ernst, M., Frølund, Bente & Smart, T. G., 2023, In: British Journal of Pharmacology. 180, 19, p. 2482-2499Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
Bavo, Francesco, Kickinger, Stefanie, Lie, M. E. K., Avgerinos, Christos, Wilhelmsen, Kristine Sloth, Wellendorph, Petrine & Frølund, Bente, 2023, In: Medicinal Chemistry Research. 32, p. 2299–2324Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- Published
Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain
Tian, Yongsong, Shehata, M. A., Gauger, Stine Juul, Ng, C. K. L., Solbak, Sara Marie Øie, Thiesen, L., Bruus-Jensen, J., Krall, J., Bundgaard, C., Gibson, K. M., Wellendorph, Petrine & Frølund, Bente, 2022, In: Journal of Medicinal Chemistry. 65, 9, p. 6656-6676Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Exploring the NCS-382 Scaffold for CaMKII alpha Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKII alpha Hub Domain
Tian, Yongsong, Shehata, M. A., Gauger, Stine Juul, Veronesi, C., Hamborg, L., Thiesen, L., Bruus-Jensen, J., Royssen, J. S., Leurs, U., Larsen, A. S. G., Krall, J., Solbak, Sara Marie Øie, Wellendorph, Petrine & Frølund, Bente, 2022, In: Journal of Medicinal Chemistry. 65, 22, p. 15066–15084Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction
Griem-Krey, Nane, Gauger, Stine Juul, Gowing, E. K., Thiesen, L., Frølund, Bente, Clarkson, A. N. & Wellendorph, Petrine, 2022, In: Biomedicine and Pharmacotherapy. 156, 10 p., 113895.Research output: Contribution to journal › Journal article › Research › peer-review
- 2021
- Published
Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors
Rostrup, F., Falk-petersen, C. B., Harpsøe, Kasper, Buchleithner, S., Conforti, I., Jung, S., Gloriam, David E., Schirmeister, T., Wellendorph, Petrine & Frølund, Bente, 22 Apr 2021, In: Journal of Medicinal Chemistry. 64, 8, p. 4730-4743 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain
Leurs, U., Klein, A. B., McSpadden, E. D., Griem-Krey, N., Solbak, S. M. Ø., Houlton, J., Villumsen, I. S., Vogensen, S. B., Hamborg, L., Gauger, S. J., Palmelund, L. B., Larsen, A. S. G., Shehata, M. A., Kelstrup, C. D., Olsen, J. V., Bach, A., Burnie, R. O., Kerr, D. S., Gowing, E. K., Teurlings, S. M. W. & 9 others, , 2021, In: Proceedings of the National Academy of Sciences of the United States of America. 118, 31, 9 p., e2108079118.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1
Kickinger, Stefanie, Lie, M. E. K., Suemasa, A., Al-Khawaja, A., Fujiwara, K., Watanabe, M., Wilhelmsen, K. S., Falk-Petersen, C. B., Frølund, Bente, Shuto, S., Ecker, G. F. & Wellendorph, Petrine, 2021, In: Frontiers in Chemistry. 9, 13 p., 736457.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors
Falk-Petersen, C. B., Rostrup, F., Löffler, R., Buchleihtner, S., Harpsøe, Kasper, Gloriam, David E., Frølund, Bente & Wellendorph, Petrine, 2021, In: Molecular Pharmacology. 100, 1, p. 46-56Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology
Griem-Krey, Nane, Frølund, Bente, Marek, A. & Wellendorph, Petrine, 2021, In: Journal of Labelled Compounds and Radiopharmaceuticals. 64, 2, 77 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based ?-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect
Bavo, Francesco, De-Jong, H., Petersen, Jonas Odgaard, Falk-Petersen, C. B., Löffler, R., Sparrow, E., Rostrup, F., Eliasen, Jannik Nicklas, Wilhelmsen, K. S., Barslund, K., Bundgaard, C., Nielsen, Birgitte, Kristiansen, Uffe, Wellendorph, Petrine, Bogdanov, Y. & Frølund, Bente, 2021, In: Journal of Medicinal Chemistry. 64, 24, p. 17795-17812Research output: Contribution to journal › Journal article › Research › peer-review
- 2020
- Published
Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors
Falk-Petersen, C. B., Tsonkov, T. M., Nielsen, M. S., Harpsøe, Kasper, Bundgaard, C., Frølund, Bente, Kristiansen, Uffe, Gloriam, David E. & Wellendorph, Petrine, 22 Jun 2020, In: Scientific Reports. 10, 1, 12 p., 10078.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
A CLASS OF SMALL-MOLECULE COMPOUNDS AND THEIR PRODRUGS FOR INTERVENTION WITH CAMK2A, AND THEIR USE IN ACUTE BRAIN INJURIES AND CENTRAL HYPERSOMNIAS
Frølund, Bente, Wellendorph, Petrine & Kornum, Birgitte Rahbek, 2020, Patent No. WO2020151795, 30 Jul 2020, Priority date 21 Jan 2019, Priority No. DK2019PA70040 20190121Research output: Patent
- Published
Compounds for the treatment of acute brain injury
Klein, A. B., Leurs, U., Houlton, J., Clausen, Rasmus Prætorius, Frølund, Bente, Clarkson, A. & Wellendorph, Petrine, 2020, Patent No. CN111989094, 24 Nov 2020, Priority date 1 Feb 2019, Priority No. PCT/DK2019/050041Research output: Patent
- Published
Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, Francesco, Loeffler, R., Damgaard, M., Ecker, G. F., Frølund, Bente & Wellendorph, Petrine, 2020, In: Scientific Reports. 10, 1, 15 p., 12992.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Sex-specific alterations in GABA receptor-mediated responses in laterodorsal tegmentum (LDT) are associated with prenatal exposure to nicotine
Eliasen, Jannik Nicklas, Krall, J., Frølund, Bente & Kohlmeier, Kristi Anne, 2020, In: Developmental Neurobiology. 80, 5-6, p. 178-199Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Silencing of spontaneous activity at α4β1/3δ GABAA receptors in hippocampal granule cells reveals different ligand pharmacology
Dalby, N. O., Falk-Petersen, C. B., Leurs, U., Scholze, P., Krall, J., Frølund, Bente & Wellendorph, Petrine, 2020, In: British Journal of Pharmacology. 177, 17, p. 3975-3990Research output: Contribution to journal › Journal article › Research › peer-review
- Published
TREATMENT OF CNS DISORDERS WITH SLEEP DISTURBANCES
Wellendorph, Petrine, Kornum, Birgitte Rahbek & Frølund, Bente, 2020, Patent No. WO2020259787 , 30 Dec 2020, Priority date 28 Jun 2019, Priority No. DK2019PA70415 20190628Research output: Patent
- Published
Unraveling the Molecular Determinants for GABA Transporter Subtype Selectivity
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, Francesco, Loffler, R., Damgaard, M., Frølund, Bente, Ecker, G. F. & Wellendorph, Petrine, 2020, p. 130A-130A.Research output: Contribution to conference › Conference abstract for conference › Research › peer-review
- 2019
- Published
Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at gamma-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters
Giraudo, A., Krall, J., Bavo, Francesco, Nielsen, Birgitte, Kongstad, Kenneth Thermann, Rolando, B., De Blasio, R., Gloriam, David E., Löffler, R., Thiesen, L., Harpsøe, Kasper, Frydenvang, Karla Andrea, Boschi, D., Wellendorph, Petrine, Lolli, M. L., Jensen, Anders A. & Frølund, Bente, 27 Jun 2019, In: Journal of Medicinal Chemistry. 62, 12, p. 5797-5809Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Synthesis and Pharmacological Evaluation of [C-11]4-Methoxy-N-[2-(thiophen-2-yl) imidazo[1,2-a] pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the delta-Subunit-Containing gamma-Aminobutyric Acid Type A Receptors
L'Estrade, E. T., Hansen, H. D., Falk-Petersen, C., Haugaard, A., Griem-Krey, Nane, Jung, S., Lueddens, H., Schirmeister, T., Erlandsson, M., Ohlsson, T., Knudsen, Gitte Moos, Herth, Matthias Manfred, Wellendorph, Petrine & Frølund, Bente, May 2019, In: ACS Omega. 4, 5, p. 8846-8851Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Lack of evidence for synaptic high-affinity γ-hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na+ -dependent SLC neurotransmitter transporters
Thiesen, L., Frølund, Bente & Wellendorph, Petrine, Apr 2019, In: Journal of Neurochemistry. 149, 2, p. 195-210 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites
Krall, J., Bavo, Francesco, Falk-Petersen, C. B., Jensen, C. H., Nielsen, J. O., Tian, Yongsong, Anglani, V., Kongstad, Kenneth Thermann, Petersen, Louise Piilgaard, Nielsen, Birgitte, Gloriam, David E., Kehler, J., Jensen, Anders A., Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 14 Mar 2019, In: Journal of Medicinal Chemistry. 62, 5, p. 2798-2813Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302625
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5-(Piperidine-4-yl)-3-hydroxypyrazole: a novel scaffold forprobing the orthosteric GABAA receptor binding site
Research output: Contribution to conference › Poster › Research
Published -
268
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Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings
Research output: Contribution to journal › Journal article › Research › peer-review
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181
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Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors
Research output: Contribution to journal › Journal article › Research › peer-review
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