Claus Juul Løland
Professor
Neuropharm and Genetics
Blegdamsvej 3
2200 København N.
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Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders
Zou, M. F., Cao, J., Abramyan, A. M., Kopajtic, T., Zanettini, C., Guthrie, D. A., Rais, R., Slusher, B. S., Shi, L., Loland, Claus Juul & Newman, A. H., Dec 2017, In: Journal of Medicinal Chemistry. 60, 24, p. 10172-10187 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A rhodamine-labeled citalopram analogue as a high-affinity fluorescent probe for the serotonin transporter
Zhang, P., Jørgensen, T. N., Loland, Claus Juul & Newman, A. H., 1 Jan 2013, In: Bioorg. Med. Chem. Lett.. 23, 1, p. 323-326 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Rational Approach to Improve Detergent Efficacy for Membrane Protein Stabilization
Yoon, S., Bae, H. E., Hariharan, P., Nygaard, Andreas, Lan, B., Woubshete, M., Sadaf, A., Liu, X., Loland, Claus Juul, Byrne, B., Guan, L. & Chae, P. S., 2024, In: Bioconjugate Chemistry. 35, 2, p. 223–231 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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X-ray structure based evaluation of analogs of citalopram: Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT
Topiol, S., Bang-Andersen, B., Sanchez, C., Plenge, P., Loland, Claus Juul, Juhl, K., Larsen, K., Bregnedal, P. & Bøgesø, K. P., 1 Feb 2017, In: Bioorganic & Medicinal Chemistry Letters. 27, 3, p. 470-478 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Type I and type II positive allosteric modulators of α7 nicotinic acetylcholine receptors induce antidepressant-like activity in mice by a mechanism involving receptor potentiation but not neurotransmitter reuptake inhibition. Correlation with mTOR intracellular pathway activation
Targowska-Duda, K. M., Budzynska, B., Michalak, A., Wnorowski, A., Loland, Claus Juul, Maj, M., Manetti, D., Romanelli, M. N., Jozwiak, K., Biala, G. & Arias, H. R., 2021, In: European Neuropsychopharmacology. 52, p. 31-47 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Neuropeptide Y Y5 receptor antagonism attenuates cocaine-induced effects in mice.
Sørensen, G., Jensen, M., Weikop, Pia, Nielsen, D. D., Christiansen, S. H. O., Loland, Claus Juul, Bengtsen, C. H., Petersen, Jørgen Holm, Fink-Jensen, Anders, Wörtwein, Gitta & Woldbye, David Paul Drucker, Feb 2012, In: Psychopharmacology. 222, p. 565-577 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Mechanism of the Association between Na+ Binding and Conformations at the Intracellular Gate in Neurotransmitter:Sodium Symporters
Stolzenberg, S., Quick, M., Zhao, C., Gotfryd, K., Khelashvili, G., Gether, Ulrik, Loland, Claus Juul, Javitch, J. A., Noskov, S., Weinstein, H. & Shi, L., 2015, In: The Journal of Biological Chemistry. 290, 22, p. 13992-4003 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
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The Environment Shapes the Inner Vestibule of LeuT
Sohail, A., Jayaraman, K., Venkatesan, S., Gotfryd, K., Daerr, M., Gether, Ulrik, Loland, Claus Juul, Wanner, K. T., Freissmuth, M., Sitte, H. H., Sandtner, W. & Stockner, T., Nov 2016, In: PLoS Computational Biology. 12, 11, 24 p., e1005197.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability
Slack, R. D., Ku, T. C., Cao, J., Giancola, J. L. B., Bonifazi, A., Loland, Claus Juul, Gadiano, A., Lam, J., Rais, R., Slusher, B. S., Coggiano, M., Tanda, G. & Newman, A. H., 2020, In: Journal of Medicinal Chemistry. 63, 5, p. 2343-2357 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A virtual high-throughput screening approach to the discovery of novel inhibitors of the bacterial leucine transporter, LeuT
Simmons, K. J., Gotfryd, K., Billesbølle, C. B., Loland, Claus Juul, Gether, Ulrik, Fishwick, C. W. G. & Johnson, A. P., Mar 2013, In: Molecular Membrane Biology. 30, 2, p. 184-94 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Biodiscoveries within the Australian plant genus Eremophila based on international and interdisciplinary collaboration: results and perspectives on outstanding ethical dilemmas
Semple, S., Stærk, Dan, Buirchell, B., Fowler, R., Gericke, Oliver, Kjaerulff, Louise, Zhao, Yong, Pedersen, H. A., Petersen, M. J., Rasmussen, L. F., Bredahl, E. K., Pedersen, Gustav Blichfeldt, McNair, Laura M., Ndi, C., Hansen, N. L., Heskes, A., Bayly, M., Loland, Claus Juul, Heinz, Nanna & Møller, Birger Lindberg, 2022, In: Plant Journal. 111, 4, p. 936-953 15866.Research output: Contribution to journal › Journal article › Research › peer-review
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Elucidating the Mechanism Behind Sodium-Coupled Neurotransmitter Transporters by Reconstitution
Schmidt, S. G., Gether, Ulrik & Loland, Claus Juul, 2022, In: Neurochemical Research. 47, p. 127–137 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Exploring the K+ binding site and its coupling to transport in the neurotransmitter: sodium symporter LeuT
Schmidt, S. G., Nygaard, Andreas, Mindell, J. A. & Loland, Claus Juul, 2024, In: eLife. 12, 21 p.Research output: Contribution to journal › Journal article › Research › peer-review
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The dopamine transporter antiports potassium to increase the uptake of dopamine
Schmidt, S. G., Malle, M. G., Nielsen, A. K., Bohr, S. S., Pugh, Ciara Frances, Nielsen, Jeppe Cederholm, Poulsen, I. H., Rand, Kasper Dyrberg, Hatzakis, Nikos & Loland, Claus Juul, 2022, In: Nature Communications. 13, 1, 12 p., 2446.Research output: Contribution to journal › Journal article › Research › peer-review
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Dynamic extracellular vestibule of human SERT: Unveiling druggable potential with high-affinity allosteric inhibitors
Salomon, K., Abramyan, A. M., Plenge, P., Wang, L., Bundgaard, C., Bang-Andersen, B., Loland, Claus Juul & Shi, L., 2023, In: Proceedings of the National Academy of Sciences of the United States of America. 120, 41, 10 p., e2304089120.Research output: Contribution to journal › Journal article › Research › peer-review
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Dendronic trimaltoside amphiphiles (DTMs) for membrane protein study
Sadaf, A., Du, Y., Santillan, C., Mortensen, Jonas Sigurd, Molist, I., Seven, A. B., Hariharan, P., Skiniotis, G., Loland, Claus Juul, Kobilka, B. K., Guan, L., Byrne, B. & Chae, P. S., 2017, In: Chemical Science. 8, 12, p. 8315-8324 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A Class of Rigid Linker-bearing Glucosides for Membrane Protein Structural Study
Sadaf, A., Mortensen, Jonas Sigurd, Capaldi, S., Tikhonova, E., Hariharan, P., de Castro Ribeiro, O., Loland, Claus Juul, Guan, L., Byrne, B. & Chae, P. S., 1 Mar 2016, In: Chemical Science. 7, 3, p. 1933-1939 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Conformationally Restricted Monosaccharide-Cored Glycoside Amphiphiles: The Effect of Detergent Headgroup Variation on Membrane Protein Stability
Sadaf, A., Ramos, M., Mortensen, Jonas Sigurd, Du, Y., Bae, H. E., Munk, C. F., Hariharan, P., Byrne, B., Kobilka, B. K., Loland, Claus Juul, Guan, L. & Chae, P. S., 2019, In: ACS chemical biology. 14, 8, p. 1717-1726 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Conformationally flexible core-bearing detergents with a hydrophobic or hydrophilic pendant: Effect of pendant polarity on detergent conformation and membrane protein stability
Sadaf, A., Kim, S., Bae, H. E., Wang, H., Nygaard, Andreas, Uegaki, Y., Du, Y., Munk, C. F., Katsube, S., Lee, H. S., Bae, J., Choi, C. W., Choi, H., Byrne, B., Gellman, S. H., Guan, L., Loland, Claus Juul, Kobilka, B. K., Im, W. & Chae, P. S., 2021, In: Acta Biomaterialia. 128, p. 393-407 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological Characterization of Purified Full-Length Dopamine Transporter from Drosophila melanogaster
Pugh, Ciara Frances, DeVree, B. T., Schmidt, S. G. & Loland, Claus Juul, 2022, In: Cells. 11, 23, 15 p., 3811.Research output: Contribution to journal › Journal article › Research › peer-review
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The mechanism of a high-affinity allosteric inhibitor of the serotonin transporter
Plenge, P., Abramyan, A. M., Sørensen, G., Mork, A., Weikop, Pia, Gether, Ulrik, Bang-Andersen, B., Shi, L. & Loland, Claus Juul, 2020, In: Nature Communications. 11, 1, 12 p., 1491.Research output: Contribution to journal › Journal article › Research › peer-review
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Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter
Plenge, P., Shi, L., Beuming, T., Te, J., Newman, A. H., Weinstein, H., Gether, Ulrik & Loland, Claus Juul, 16 Nov 2012, In: The Journal of Biological Chemistry. 287, 47, p. 39316-26 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
Plenge, P., Yang, D., Salomon, K., Laursen, L., Kalenderoglou, I. E., Newman, A. H., Gouaux, E., Coleman, J. A. & Loland, Claus Juul, 2021, In: Nature Communications. 12, 1, 12 p., 5063.Research output: Contribution to journal › Journal article › Research › peer-review
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A Conserved Salt Bridge between Transmembrane Segment 1 and 10 Constitutes an Extracellular Gate in the Dopamine Transporter
Pedersen, A. V., Andreassen, T. F. & Loland, Claus Juul, 2014, In: Journal of Biological Chemistry. 289, 50, p. 35003-350014 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Elucidation of Structural Elements for Selectivity across Monoamine Transporters: Novel 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues
Okunola-Bakara, O., Cao, J., Kopajtic, T., Katz, J. L., Loland, Claus Juul, Shi, L. & Newman, A. H., 2014, In: Journal of Medicinal Chemistry. 57, 3, p. 1000-1013 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile
Okorom, A. V., Camacho-Hernandez, G. A., Salomon, Kristine Walløe, Lee, K. H., Ku, T. C., Cao, J., Won, S. J., Friedman, J., Lam, J., Paule, J., Rais, R., Klein, B., Xi, Z. X., Shi, L., Loland, Claus Juul & Newman, A. H., 2024, In: Journal of Medicinal Chemistry. 67, 1, p. 709-727 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structural probing of a microdomain in the dopamine transporter by engineering of artificial Zn2+ binding sites
Norregaard, L., Visiers, I., Loland, Claus Juul, Ballesteros, J. A., Weinstein, H. & Gether, Ulrik, 2001, In: Biochemistry. 39 (51), p. 15836-15846Research output: Contribution to journal › Journal article › Research › peer-review
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Evidence for distinct sodium-, dopamine-, cocaine-dependent conformational changes in transmembrane segments 7 and 8 of the dopamine
Norregaard, L., Loland, Claus Juul & Gether, Ulrik, 2003, In: Journal of Biological Chemistry. Vol. 278 (33), p. 30587-96Research output: Contribution to journal › Journal article › Research › peer-review
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Evidence for distinct sodium-, dopamine-, and cocaine-dependent conformational changes in transmembrane segments 7 and 8 of the dopamine transporter
Norregaard, L., Loland, Claus Juul & Gether, Ulrik, 15 Aug 2003, In: The Journal of Biological Chemistry. 278, 33, p. 30587-96 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structural probing of a microdomain in the dopamine transporter by engineering of artificial Zn2+ binding sites
Norregaard, L., Visiers, I., Loland, Claus Juul, Ballesteros, J., Weinstein, H. & Gether, Ulrik, 26 Dec 2000, In: Biochemistry. 39, 51, p. 15836-15846 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Substrate-Induced Conformational Dynamics of the Dopamine Transporter
Nielsen, A. K., Moller, I. R., Rasmussen, Søren Gøgsig Faarup, Rand, Kasper Dyrberg & Loland, Claus Juul, 2019, In: Biophysical Society. Annual Meeting. Abstracts. 116, 3, p. 346A 1 p., 1714-Pos.Research output: Contribution to journal › Conference abstract in journal › Research › peer-review
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Substrate-induced conformational dynamics of the dopamine transporter
Nielsen, A. K., Möller, I. R., Wang, Y., Rasmussen, Søren Gøgsig Faarup, Lindorff-Larsen, Kresten, Rand, Kasper Dyrberg & Loland, Claus Juul, 2019, In: Nature Communications. 10, 14 p., 2714.Research output: Contribution to journal › Journal article › Research › peer-review
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Persistent binding at dopamine transporters determines sustained psychostimulant effects
Niello, M., Sideromenos, S., Gradisch, R., O'Shea, R., Schwazer, J., Maier, J., Kastner, N., Sandtner, W., Jäntsch, K., Lupica, C. R., Hoffman, A. F., Lubec, G., Loland, Claus Juul, Stockner, T., Pollak, D. D., Baumann, M. H. & Sitte, H. H., 2023, In: Proceedings of the National Academy of Sciences of the United States of America. 120, 6, 11 p., e2114204120.Research output: Contribution to journal › Journal article › Research › peer-review
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Allosteric Modulation of Neurotransmitter Transporters as a Therapeutic Strategy
Niello, M., Gradisch, R., Loland, Claus Juul, Stockner, T. & Sitte, H. H., 2020, In: Trends in Pharmacological Sciences. 41, 7, p. 446-463 18 p.Research output: Contribution to journal › Review › Research › peer-review
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Improving the Sequence Coverage of Integral Membrane Proteins during Hydrogen/Deuterium Exchange Mass Spectrometry Experiments
Möller, I. R., Slivacka, M., Hausner, J., Nielsen, A. K., Pospisilova, E., Rand, Kasper Dyrberg, Liskova, R., Polak, M., Loland, Claus Juul, Kadek, A., Man, P. & Rand, Kasper Dyrberg, 2019, In: Analytical Chemistry. 91, 17, p. 10970-10978 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Conformational dynamics of the human serotonin transporter during substrate and drug binding
Möller, I. R., Slivacka, M., Nielsen, A. K., Rasmussen, Søren Gøgsig Faarup, Gether, Ulrik, Loland, Claus Juul & Rand, Kasper Dyrberg, 11 Apr 2019, In: Nature Communications. 10, 1, 1687.Research output: Contribution to journal › Journal article › Research › peer-review
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Probing the conformational impact of detergents on the integral membrane protein LeuT by global HDX-MS
Möller, I. R., Merkle, P. S., Calugareanu, D., Comamala, G., Schmidt, S. G., Loland, Claus Juul & Rand, Kasper Dyrberg, 2020, In: Journal of Proteomics. 225, 103845.Research output: Contribution to journal › Journal article › Research › peer-review
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Short-Range Distance Measurement by Transition Metal Ion FRET
Mortensen, Jonas Sigurd & Loland, Claus Juul, 2020, Biophysics of membrane proteins. Humana Press, p. 299-311 13 p. (Methods in Molecular Biology, Vol. 2168).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Substrate-modulated unwinding of transmembrane helices in the NSS transporter LeuT: Recommended in F1000Prime as being of special significance in its field by F1000 Faculty Member Robert Vandenberg
Merkle, P. S., Gotfryd, K., Cuendet, M. A., Leth-Espensen, K. Z., Gether, Ulrik, Loland, Claus Juul & Rand, Kasper Dyrberg, 2018, In: Science Advances. 4, 5, 12 p., eaar6179.Research output: Contribution to journal › Journal article › Research › peer-review
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Partial Unwinding of Transmembrane Helices Facilitates Alternating Access in the Neurotransmitter: Sodium Symporter LeuT
Merkle, P. S., Gotfryd, K., Cuendet, M. A., Leth-Espensen, K. Z., Gether, Ulrik, Loland, Claus Juul & Rand, Kasper Dyrberg, 28 Jun 2017Research output: Other contribution › Research
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Engineered Zn(2+)switches in the gamma-aminobutyric acid (GABA) transporter-1. Differential effects on GABA uptake and currents
MacAulay, Nanna, Bendahan, A., Loland, Claus Juul, Zeuthen, Thomas, Kanner, B. I. & Gether, Ulrik, 2001, In: Journal of Biological Chemistry. 276, p. 40476-40485Research output: Contribution to journal › Journal article › Research › peer-review
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The use of LeuT as a model in elucidating binding sites for substrates and inhibitors in neurotransmitter transporters
Loland, Claus Juul, Mar 2015, In: BBA General Subjects. 1850, 3, p. 500-510 11 p.Research output: Contribution to journal › Review › Research › peer-review
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Defining proximity relationships in the tertiary structure of the dopamine transporter. Identification of a conserved glutamic acid as a third coordinate in the endogenous Zn(2+)-binding site.
Loland, Claus Juul, Norregaard, L. & Gether, Ulrik, 1999, In: Journal of Biological Chemistry. 274, 52, p. 36928-34 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Relationship between conformational changes in the dopamine transporter and cocaine-like subjective effects of uptake inhibitors.
Loland, Claus Juul, Desai, R. I., Zou, M., Cao, J., Grundt, P., Gerstbrein, K., Sitte, H. H., Newman, A. H., Katz, J. L. & Gether, Ulrik, 2007, In: Molecular Pharmacology. 73, 3, p. 813-23 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Intracellular residues in the dopamine transporter critical for conformational isomerization, molecular gating and cocaine binding
Loland, Claus Juul, Granas, C., Javitc, J. & Gether, Ulrik, 2004, In: Journal of Biological Chemistry. Vol. 279, no. 5, p. 3228-38Research output: Contribution to journal › Journal article › Research › peer-review
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Insights from endogenous and engineered Zn2+-binding sites in monoanine transporters
Loland, Claus Juul & Gether, Ulrik, 2004, Molecular Neuropharmacology: Strategies and Methods. p. 191-213Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
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Probing dopamine transporter structure and function y Zn2+ site engineering
Loland, Claus Juul, Nørgaard-Nielsen, K. & Gether, Ulrik, 2003, In: European Journal of Pharmacology. Vol. 479, no 1-3, p. 187-97Research output: Contribution to journal › Review › Research › peer-review
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Generation of an activating ZN(2+) switch in the dopamine transporter: Mutation of an intracellular tyrosine constitutively alters the conformational equilibrium of the transport cycle
Loland, Claus Juul, Norregaard, L., Litman, Thomas & Gether, Ulrik, 2002, In: Proceedings of the National Academy of Science of the United States of America. vol. 99(3), p. 1683-8Research output: Contribution to journal › Journal article › Research › peer-review
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Neurotransmitter transporters: structure and function
Loland, Claus Juul & Gether, Ulrik, 2009, Texbook of Drug Design and Discovery. Madsen, U., Krogsgaard-Larsen, P. & Stromgaard, K. (eds.). 4 ed. Taylor & FrancisResearch output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
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Neurotransmitter Transporters: Structure, Function, and Drug Binding
Loland, Claus Juul & Gether, Ulrik, 2017, Textbook of Drug Design and Discovery. Stromgaard, K., Krogsgaard-Larsen, P. & Madsen, U. (eds.). 5 ed. Boca Raton: CRC Press, p. 233-248 16 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
ID: 4359
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Grafted biomembranes containing membrane proteins – the case of the leucine transporter
Research output: Contribution to journal › Journal article › Research › peer-review
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226
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Direct assessment of substrate binding to the Neurotransmitter:Sodium Symporter LeuT by solid state NMR
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195
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A Class of Rigid Linker-bearing Glucosides for Membrane Protein Structural Study
Research output: Contribution to journal › Journal article › Research › peer-review
Published