Browse by Research Team

2025

Pharmacological characterization of a clinical candidate, TG-0054, a small molecule inverse agonist targeting CXCR4.
Pan, K.S., Wang, Z., Pfeil, C., Bergkamp, N.D., Mobach, S., Roth, S., Rizk, A., Lohse, M.J., Annibale, P., Siderius, M., Zimmermann, M., Smit, M.J. and Bosma, R.
Molecular Pharmacology 107 (4): 100015. April 2025

Effects of altered gravity on adrenergic-mediated cAMP signalling in intact cells.
Bathe-Peters, M., Sohail, I., Sirbu, A., Schneider, K., Patriarchi, T., De Lanerolle, P. and Annibale, P.
bioRxiv : 2025.03.02.640942. 3 March 2025

Pharmacological characterisation of a clinical candidate, TG-0054, a small molecule inverse agonist targeting CXCR4.
Pan, K.S., Wang, Z., Pfeil, C., Bergkamp, N.D., Mobach, S., Roth, S., Rizk, A., Lohse, M.J., Annibale, P., Siderius, M., Zimmermann, M., Smit, M.J. and Bosma, R.
Molecular Pharmacology : 100015. 31 January 2025 (In Press)

2024

Disruption of basal CXCR4 oligomers impairs oncogenic properties in lymphoid neoplasms.
Mobach, S, Bergkamp, N.D., Ma, Z, Haselager, M.V., Anbuhl, S.M., Jurriens, D, van den Bor, J., Wang, Z., Crudden, C., Roos, J.L., Perez Almeria, C.V., Boergonje, R.A., Lohse, M.J., Bosma, R., Eldering, E., Siderius, M., Wu, W., Spaargaren, M., Tonino, S.H., Kater, A.P., Smit, M.J. and Heukers, R.
bioRxiv : 2024.12.06.627249. 7 December 2024

MRAP2 modifies the signaling and oligomerization state of the melanocortin-4 receptor.
Sohai, I., Laurin, S.A., Kleinau, G., Chunilal, V., Morton, A., Kagiali, Z.C.U., Tello, J.A., Lohse, M.J., Scheerer, P., Bouvier, M., McCormick, P., Annibale, P. and Biebermann, H.
bioRxiv : 2024.04.09.588099v3. 5 October 2024

Cell swelling enhances ligand-driven β-adrenergic signaling.
Sirbu, A., Bathe-Peters, M., Kumar, J.L.M, Inoue, A., Lohse, M.J. and Annibale, P.
Nature Communications 15 (1): 7822. 7 September 2024

Cell swelling enhances canonical β-adrenergic signaling.
Sirbu, A., Bathe-Peters, M., Kumar, J.L.M., Inoue, A., Lohse, M. and Annibale, P.
bioRxiv : 2023.06.23.544496v5. 23 August 2024

The C-terminus of the prototypical M2 muscarinic receptor localizes to the mitochondria and regulates cell respiration under stress conditions.
Fasciani, I., Petragnano, F., Wang, Z., Edwards, R., Telugu, N., Pietrantoni, I., Zabel, U., Zauber, H., Grieben, M., Terzenidou, M.E., Di Gregorio, J., Pellegrini, C., Santini, S., Taddei, A.R., Pohl, B., Aringhieri, S., Carli, M., Aloisi, G., Marampon, F., Charlesworth, E., Roman, A., Diecke, S., Flati, V., Giorgi, F., Amicarelli, F., Tobin, A.B., Scarselli, M., Tokatlidis, K., Rossi, M., Lohse, M.J., Annibale, P. and Maggio, R.
PLoS Biology 22 (4): e3002582. 29 April 2024

ADAM19 cleaves the PTH receptor and associates with brachydactyly type E.
Aydin, A., Klenk, C., Nemec, K., Işbilir, Ali, Martin, L.M., Zauber, H., Rrustemi, T., Toka, H.R., Schuster, H., Gong, M., Stricker, S., Bock, A., Bähring, S., Selbach, M., Lohse, M.J. and Luft, F.C.
Life Science Alliance 7 (4): e202302400. April 2024

Impairment of the adrenergic reserve associated with exercise intolerance in a murine model of heart failure with preserved ejection fraction.
Semmler, L., Jeising, T., Huettemeister, J., Bathe-Peters, M., Georgoula, K., Roshanbin, R., Sander, P., Fu, S., Bode, D., Hohendanner, F., Pieske, B., Annibale, P., Schiattarella, G.G., Oeing, C.U. and Heinzel, F.R.
Acta Physiologica 240 (4): e14124. April 2024

Fluorescent tools for the imaging of dopamine D2-like receptors.
Nagl, M., Moennich, D., Rosier, N., Schihada, H., Sirbu, A., Konar, N., Reyes-Resina, I., Navarro, G., Franco, R., Kolb, P., Annibale, P. and Pockes, S.
ChemBioChem 25 (2): e202300659. 15 January 2024

Shedding light on the D1‐like receptors: a fluorescence‐based toolbox for visualization of the D1 and D5 receptors.
Rosier, N., Moennich, D., Nagl, M., Schihada, H., Sirbu, A., Konar, N., Reyes-Resina, I., Navarro, G., Franco, R., Kolb, P., Annibale, P. and Pockes, S.
ChemBioChem 25 (2): e202300658. 15 January 2024

2023

Quantitative morphological analysis of the T-tubular network of ventricular cardiomyocytes using novel image processing tools.
Georgoula, K., Sage, D. and Annibale, P.
In: European Conferences on Biomedical Optics 2023, 25-29 June 2023, Munich, Germany. 11 August 2023

Spatiotemporal GPCR signaling illuminated by genetically encoded fluorescent biosensors.
Kayser, C., Melkes, B., Derieux, C. and Bock, A.
Current Opinion in Pharmacology 71 : 102384. August 2023

2022

Evaluation of pharmacological rescue of melanocortin-4 receptor nonsense mutations by aminoglycoside.
Höpfner, F., Paisdzior, S., Reininghaus, N., Sohail, I., Scheerer, P., Annibale, P., Biebermann, H. and Kühnen, P.
Life 12 (11): 1793. 5 November 2022

Fluorescence spectroscopy of low-level endogenous β-adrenergic receptor expression at the plasma membrane of differentiating human iPSC-derived cardiomyocytes.
Gmach, P., Bathe-Peters, M., Telugu, N., Miller, D.C. and Annibale, P.
International Journal of Molecular Sciences 23 (18): 10405. 8 September 2022

Development of an indole-amide-based photoswitchable cannabinoid receptor subtype 1 (CB(1)R) "Cis-On" agonist.
Rodríguez-Soacha, D.A., Steinmüller, S.A.M., Işbilir, A., Fender, J., Deventer, M.H., Ramírez, Y.A., Tutov, A., Sotriffer, C., Stove, C.P., Lorenz, K., Lohse, M.J., Hislop, J.N. and Decker, M.
ACS Chemical Neuroscience 13 (16): 2410-2435. 17 August 2022

Functional modulation of PTH1R activation and signaling by RAMP2.
Nemec, K., Schihada, H., Kleinau, G., Zabel, U., Grushevsky, E.O., Scheerer, P., Lohse, M.J. and Maiellaro, I.
Proceedings of the National Academy of Sciences of the United States of America 119 (32): e2122037119. 9 August 2022

The impact of membrane protein diffusion on GPCR signaling.
Boltz, H.H., Sirbu, A., Stelzer, N., de Lanerolle, P., Winkelmann, S. and Annibale, P.
Cells 11 (10): 1660. 17 May 2022

Receptor-associated independent cAMP nanodomains mediate spatiotemporal specificity of GPCR signaling.
Anton, S.E., Kayser, C., Maiellaro, I., Nemec, K., Möller, J., Koschinski, A., Zaccolo, M., Annibale, P., Falcke, M., Lohse, M.J. and Bock, A.
Cell 185 (7): 1130-1142.e11. 31 March 2022

Unraveling the hidden temporal range of fast β(2)-adrenergic receptor mobility by time-resolved fluorescence.
Balakrishnan, A., Hemmen, K., Choudhury, S., Krohn, J.H., Jansen, K., Friedrich, M., Beliu, G., Sauer, M., Lohse, M.J. and Heinze, K.G.
Communications Biology 5 (1): 176. 28 February 2022

Proteolytic cleavage of the extracellular domain affects signaling of parathyroid hormone 1 receptor.
Klenk, C., Hommers, L. and Lohse, M.J.
Frontiers in Endocrinology 13 : 839351. 22 February 2022

Real-time measurements of intracellular cAMP gradients using FRET-based cAMP nanorulers.
Kayser, C., Lohse, M.J. and Bock, A.
Methods in Molecular Biology 2483 : 1-13. 2022

2021

Dual-color fluorescence cross-correlation spectroscopy to study protein-protein interaction and protein dynamics in live cells.
Hemmen, K., Choudhury, S., Friedrich, M., Balkenhol, J., Knote, F., Lohse, M.J. and Heinze, K.G.
Journal of Visualized Experiments 178 : e62954. 11 December 2021

Viewpoints on the first transatlantic GPCR symposium for early-career investigators.
Bender, B.J., Bock, A., Nesheva, D.N. and Perry-Hauser, N.A.
ACS Pharmacology & Translational Science 4 (5): 1705-1711. 8 October 2021

A versatile sub-nanomolar fluorescent ligand enables NanoBRET binding studies and single-molecule microscopy at the histamine H(3) receptor.
Rosier, N., Grätz, L., Schihada, H., Möller, J., Işbilir, A., Humphrys, L.J., Nagl, M., Seibel, U., Lohse, M.J. and Pockes, S.
Journal of Medicinal Chemistry 64 (15): 11695-11708. 12 August 2021

Visualization of β-adrenergic receptor dynamics and differential localization in cardiomyocytes.
Bathe-Peters, M., Gmach, P., Boltz, H.H., Einsiedel, J., Gotthardt, M., Hübner, H., Gmeiner, P., Lohse, M.J. and Annibale, P.
Proceedings of the National Academy of Sciences of the United States of America 118 (23): e2101119118. 8 June 2021

Differences in interactions between transmembrane domains tune the activation of metabotropic glutamate receptors.
Thibado, J.K, Tano, J.Y., Lee, J., Salas-Estrada, L., Provasi, D., Strauss, A., Ribeiro, J.M.L., Xiang, G., Broichhagen, J., Filizola, M., Lohse, M.J. and Levitz, J.
eLife 10 : e67027. 21 April 2021

Quantitative spectroscopy of single molecule interaction times.
Boltz, H.H., Sirbu, A., Stelzer, N., Lohse, M.J., Schütte, C. and Annibale, P.
Optics Letters 46 (7): 1538-1541. 1 April 2021

Allosteric coupling and biased agonism in G protein-coupled receptors.
Bock, A. and Bermudez, M.
FEBS Journal 288 (8): 2513-2528. April 2021

Atypical antipsychotics and metabolic syndrome: from molecular mechanisms to clinical differences.
Carli, M., Kolachalam, S., Longoni, B., Pintaudi, A., Baldini, M., Aringhieri, S., Fasciani, I., Annibale, P., Maggio, R. and Scarselli, M.
Pharmaceuticals 14 (3): 238. March 2021

Determination of G-protein-coupled receptor oligomerization by molecular brightness analyses in single cells.
Işbilir, A., Serfling, R., Möller, J., Thomas, R., De Faveri, C., Zabel, U., Scarselli, M., Beck-Sickinger, A.G., Bock, A., Coin, I., Lohse, M.J. and Annibale, P.
Nature Protocols 16 (3): 1419-1451. March 2021

Structural and functional characterization of allatostatin receptor type-C of Thaumetopoea pityocampa, a potential target for next-generation pest control agents.
Shahraki, A., Işbilir, A., Dogan, B., Lohse, M.J., Durdagi, S. and Birgul-Iyison, N.
Journal of Chemical Information and Modeling 61 (2): 715-728. 22 February 2021

Bioluminescence in G protein-coupled receptors drug screening using nanoluciferase and halo-tag technology.
Schihada, H., Nemec, K., Lohse, M.J. and Maiellaro, I.
Methods in Molecular Biology 2268 : 137-147. 2021

2020

Pharmacological characterization of the stick insect Carausius morosus allatostatin-C receptor with its endogenous agonist.
Işbilir, A., Duan Sahbaz, B., Tuncgenc, G., Bünemann, M., Lohse, M.J. and Birgül-Iyison, N.
ACS Omega 5 (50): 32183-32194. 22 December 2020

The role of orthosteric building blocks of bitopic ligands for muscarinic M1 receptors.
Volpato, D., Kauk, M., Messerer, R., Bermudez, M., Wolber, G., Bock, A., Hoffmann, C. and Holzgrabe, U.
ACS Omega 5 (49): 31706-31715. 15 December 2020

Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists.
Işbilir, A., Möller, J., Arimont, M., Bobkov, V., Perpiñá-Viciano, C., Hoffmann, C., Inoue, A., Heukers, R., de Graaf, C., Smit, M.J., Annibale, P. and Lohse, M.J.
Proceedings of the National Academy of Sciences of the United States of America 117 (46): 29144-29154. 17 November 2020

Ligand-specific allosteric coupling controls G-protein-coupled receptor signaling.
Holze, J., Bermudez, M., Pfeil, E.M., Kauk, M., Bödefeld, T., Irmen, M., Matera, C., Dallanoce, C., De Amici, M., Holzgrabe, U., König, G.M., Tränkle, C., Wolber, G., Schrage, R., Mohr, K., Hoffmann, C., Kostenis, E. and Bock, A.
ACS Pharmacology & Translational Science 3 (5): 859-867. 9 October 2020

Optical mapping of cAMP signaling at the nanometer scale.
Bock, A., Annibale, P., Konrad, C., Hannawacker, A., Anton, S.E., Maiellaro, I., Zabel, U., Sivaramakrishnan, S., Falcke, M. and Lohse, M.J.
Cell 182 (6): 1519-1530. 17 September 2020

Single-molecule analysis reveals agonist-specific dimer formation of µ-opioid receptors.
Möller, J., Isbilir, A., Sungkaworn, T., Osberg, B., Karathanasis, C., Sunkara, V., Grushevskyi, E.O., Bock, A., Annibale, P., Heilemann, M., Schütte, C. and Lohse, M.J.
Nature Chemical Biology 16 (9): 946-954. September 2020

Establishing a sensitive fluorescence-based quantification method for cyclic nucleotides.
Gruteser, N., Kohlhas, V., Balfanz, S., Franzen, A., Günther, A., Offenhäusser, A., Müller, F., Nikolaev, V., Lohse, M.J. and Baumann, A.
BMC Biotechnology 20 (1): 47. 27 August 2020

Kinetic analysis of the early signaling steps of the human chemokine receptor CXCR4.
Perpina-Viciano, C., Işbilir, A., Zarca, A., Caspar, B., Kilpatrick, L.E., Hill, S.J., Smit, M.J., Lohse, M.J. and Hoffmann, C.
Molecular Pharmacology 98 (2): 72-87. August 2020

Unmasking features of the auto-epitope essential for β(1)-adrenoceptor activation by autoantibodies in chronic heart failure.
Wölfel, A., Sättele, M., Zechmeister, C., Nikolaev, V.O., Lohse, M.J., Boege, F., Jahns, R. and Boivin-Jahns, V.
ESC Heart Failure 7 (4): 1830-1841. August 2020

Development of a conformational histamine H(3) receptor biosensor for the synchronous screening of agonists and inverse agonists.
Schihada, H., Ma, X., Zabel, U., Vischer, H.F., Schulte, G., Leurs, R., Pockes, S. and Lohse, M.J.
ACS Sensors 5 (6): 1734-1742. 26 June 2020

Visualizing the functional 3D shape and topography of long noncoding RNAs by single-particle atomic force microscopy and in-solution hydrodynamic techniques.
Uroda, T., Chillón, I., Annibale, P., Teulon, J.M., Pessey, O., Karuppasamy, M., Pellequer, J.L. and Marcia, M.
Nature Protocols 15 (6): 2107-2139. June 2020

Linescan microscopy data to extract diffusion coefficient of a fluorescent species using a commercial confocal microscope.
Bathe-Peters, M., Gmach, P., Annibale, P. and Lohse, M.J.
Data in Brief 29 : 105063. April 2020

Spatial heterogeneity in molecular brightness.
Annibale, P. and Lohse, M.J.
Nature Methods 17 (3): 273-275. March 2020

Differential signaling profiles of MC4R mutations with three different ligands.
Paisdzior, S., Dimitriou, I.M., Schöpe, P.C., Annibale, P., Scheerer, P., Krude, H., Lohse, M.J., Biebermann, H. and Kühnen, P.
International Journal of Molecular Sciences 21 (4): 1224. 12 February 2020

Hypnotika und Sedativa.
Lohse, M.J.
In: Arzneiverordnungs-Report 2020 : Aktuelle Daten, Kosten, Trends und Kommentare. Springer, Berlin, Heidelberg, 571-582. ISBN 978-3-662-62167-7 2020

Ophthalmika.
Lohse, M.J.
In: Arzneiverordnungs-Report 2020 : Aktuelle Daten, Kosten, Trends und Kommentare. Springer, Berlin, Heidelberg, 733-758. ISBN 978-3-662-62168-4 2020

Psychopharmaka.
Lohse, M.J.
In: Arzneiverordnungs-Report 2020 : Aktuelle Daten, Kosten, Trends und Kommentare. Springer, Berlin, Heidelberg, 781-814. ISBN 978-3-662-62168-4 2020

2019

Context-dependent signaling of CXC chemokine receptor 4 and atypical chemokine receptor 3.
Heuninck, J., Perpina Viciano, C., Işbilir, A., Caspar, B., Capoferri, D., Briddon, S.J., Durroux, T., Hill, S.J., Lohse, M.J., Milligan, G., Pin, J.P. and Hoffmann, C.
Molecular Pharmacology 96 (6): 778-793. December 2019

Vibrational spectroscopy as a powerful tool for follow-up immunoadsorption therapy treatment of dilated cardiomyopathy - a case report.
Huang, J., Ramoji, A., Guo, S., Bocklitz, T., Boivin-Jahns, V., Möller, J., Kiehntopf, M., Noutsias, M., Popp, J. and Neugebauer, U.
Analyst 145 (2): 486-496. 15 November 2019

Conserved pseudoknots in lncRNA MEG3 are essential for stimulation of the p53 pathway.
Uroda, T., Anastasakou, E., Rossi, A., Teulon, J.M., Pellequer, J.L., Annibale, P., Pessey, O., Inga, A., Chillón, I. and Marcia, M.
Molecular Cell 75 (5): 982-995. 5 September 2019

Quantitative single-residue bioorthogonal labeling of G protein-coupled receptors in live cells.
Serfling, R., Seidel, L., Bock, A., Lohse, M.J., Annibale, P. and Coin, I.
ACS Chemical Biology 14 (6): 1141-1149. 21 June 2019

Stepwise activation of a class C GPCR begins with millisecond dimer rearrangement.
Grushevskyi, E.O., Kukaj, T., Schmauder, R., Bock, A., Zabel, U., Schwabe, T., Benndorf, K. and Lohse, M.J.
Proceedings of the National Academy of Sciences of the United States of America 116 (20): 10150-10155. 14 May 2019

Does divergent binding pocket closure drive ligand bias for class A GPCRs?
Bermudez, M. and Bock, A.
Trends in Pharmacological Sciences 40 (4): 236-239. April 2019

All-in-one confocal and widefield fluorescence microscope to investigate membrane receptor dynamics.
Bathe-Peters, M., Gmach, P., Annibale, P. and Lohse, M.J.
In: Imaging and Applied Optics Congress 2019 (COSI, IS, MATH, pcAOP), 24-27 Jun 2019, Munich, Germany. 2019

2018

A functional genetic variation of SLC6A2 repressor hsa-miR-579-3p upregulates sympathetic noradrenergic processes of fear and anxiety.
Hommers, L.G., Richter, J., Yang, Y., Raab, A., Baumann, C., Lang, K., Schiele, M.A., Weber, H., Wittmann, A., Wolf, C., Alpers, G.W., Arolt, V., Domschke, K., Fehm, L., Fydrich, T., Gerlach, A., Gloster, A.T., Hamm, A.O., Helbig-Lang, S., Kircher, T., Lang, T., Pané-Farré, C.A., Pauli, P., Pfleiderer, B., Reif, A., Romanos, M., Straube, B., Ströhle, A., Wittchen, H.U., Frantz, S., Ertl, G., Lohse, M.J., Lueken, U. and Deckert, J.
Translational Psychiatry 8 (1): 226. 19 October 2018

A universal bioluminescence resonance energy transfer sensor design enables high-sensitivity screening of GPCR activation dynamics.
Schihada, H., Vandenabeele, S., Zabel, U., Frank, M., Lohse, M.J. and Maiellaro, I.
Communications Biology 1 : 105. 7 August 2018

Allosteric modulators targeting CNS muscarinic receptors.
Bock, A., Schrage, R. and Mohr, K.
Neuropharmacology 136 (Part C): 427-437. 1 July 2018

A panoramic view on GPCRs: the 1st Berlin Symposium for Interdisciplinary GPCR research.
Bock, A. and Bermudez, M.
Naunyn-Schmiedeberg's Archives of Pharmacology 391 (7): 769-771. July 2018

Molecular details of dimerization kinetics reveal negligible populations of transient µ-opioid receptor homodimers at physiological concentrations.
Meral, D., Provasi, D., Prada-Gracia, D., Möller, J., Marino, K., Lohse, M.J. and Filizola, M.
Scientific Reports 8 (1): 7705. 16 May 2018

Increased fear learning, spatial learning as well as neophobia in Rgs2(-/-) mice.
Raab, A., Popp, S., Lesch, K.P., Lohse, M.J., Fischer, M., Deckert, J. and Hommers, L.
Genes Brain and Behavior 17 (4): e12420. April 2018

All-optical microscope autofocus based on an electrically tunable lens and a totally internally reflected IR laser.
Bathe-Peters, M., Annibale, P. and Lohse, M.J.
Optics Express 26 (3): 2359-2368. 5 February 2018

Related GPCRs couple differently to G(s): preassociation between G protein and 5-HT(7) serotonin receptor reveals movement of Gα(s) upon receptor activation.
Andressen, K.W., Ulsund, A.H., Krobert, K.A., Lohse, M.J., Buenemann, M. and Levy, F.O.
FASEB Journal 32 (2): 1059-1069. 5 February 2018

2017

Visualization of class A GPCR oligomerization by image-based fluorescence fluctuation spectroscopy.
Isbilir, A., Moeller, J., Bock, A., Zabel, U., Annibale, P. and Lohse, M.J.
bioRxiv : 240903. 29 December 2017

Evolutionary action and structural basis of the allosteric switch controlling β(2)AR functional selectivity.
Schönegge, A.M., Gallion, J., Picard, L.P., Wilkins, A.D., Le Gouill, C., Audet, M., Stallaert, W., Lohse, M.J., Kimmel, M., Lichtarge, O. and Bouvier, M.
Nature Communications 8 (1): 2169. 18 December 2017

Single-molecule imaging reveals receptor-G protein interactions at cell surface hot spots.
Sungkaworn, T., Jobin, M.L., Burnecki, K., Weron, A., Lohse, M.J. and Calebiro, D.
Nature 550 (7677): 543-547. 26 October 2017

Mapping the dynamics of the glucocorticoid receptor within the nuclear landscape.
Stortz, M., Presman, D.M., Bruno, L., Annibale, P., Dansey, M.V., Burton, G., Gratton, E., Pecci, A. and Levi, V.
Scientific Reports 7 (1): 6219. 24 July 2017

Ligand-specific restriction of extracellular conformational dynamics constrains signaling of the M(2) muscarinic receptor.
Bermudez, M., Bock, A., Krebs, F., Holzgrabe, U., Mohr, K., Lohse, M.J. and Wolber, G.
ACS Chemical Biology 12 (7): 1743-1748. 21 July 2017

Is signaling specificity encoded in arrestin conformation?
Hoffmann, C., Lohse, M.J. and Luttrell, L.M.
In: The Structural Basis of Arrestin Functions. Springer, Cham, Switzerland, 235-253. ISBN 978-3-319-57552-0 25 May 2017

Was ist in der Medizin moeglich: Neue Therapien.
Lohse, M.
In: Medizin 4.0 - Zur Zukunft der digitalisierten Welt. IV. Interdisziplinaerer Kongress Berlin 2016 mit der Heinz Nixdorf-Stiftung - gemeinsam mit der Charite - Universitaetsmedizin Berlin, 1-2 June 2016, Berlin, Germany. 2017