© EIMI/P. Leßmann

Chemical Targeting Lab (Dr. Andreas Faust)

In our chemical and radiochemical laboratories, we develop new tracers for diagnostic molecular imaging using positron emission tomography (PET), single-photon emission tomography (SPECT), optical and photoacoustic imaging. On the one hand, we focus on specific ligands for the alarmins S100A8/S100A9; on the other hand, we work on bacteria-specific tracers based on complex carbohydrates or siderophores. Various short-lived nuclides such as the positron emitter fluorine-18 or the gamma emitter technetium-99m are used. In our workgroup we also develop absorbers for improved photoacoustic imaging.

  • Research News & Views

  • Projects

    Distribution of immune cells in the body of a mouse, imaged with optical imaging
    © S. Gran & L. Honold et al./Theranostics 2018(8)

    Immune-Image

    In this project, we develop methods for monitoring immune cells before, during and after immune treatment. Initially, we will look at these processes in animal models for different diseases – with the aim of translating the results and methods to patients mid-term enabling us to establish image-guided immunotherapies with improved efficacy in diseases such as cancer or inflammation.

    Coordinator: Albert D. Windhorst (Amsterdam University Medical Centre, the Netherlands)
    EIMI members involved as partners: Michael Schäfers, Andreas Jacobs, Andreas Faust, Sven Hermann, Friedemann Kiefer, Sabine Stötzer
    Project term: 10/2019 - 09/2024
    Project number: Innovative Medicines Initiative 2 Joint Undertaking, grant agreement No 831514

    Vascular graft infection with S. aureus
    © EIMI

    Bacterial vascular graft infections – impact of sterile inflammation and tissue injury on biofilm formation and bacterially elicited processes

    Vascular graft infection is a rare but very severe complication with a high death rate, and there are currently no reliable diagnostic tools. Newly developed tracers are intended to enable detecting bacterial distribution in the body at early time points after the infection using PET imaging.

    Principal investigators: Andreas Faust (EIMI), Silke Niemann
    Project term:     01/2017 - 06/2020
    Project number:     Fau2/014/17 | Medical Faculty, University of Münster

  • Team

  • Publications

    2021

    Axer A, Jumde RP, Adam S, Faust A, Schäfers M, Fobker M, Koehnke J, Hirsch AKH, Gilmour R. Enhancing glycan stability via site-selective fluorination: modulating substrate orientation by molecular design. Chem. Sci. 2021;12: 1286-1294. Abstract
    Maisuls I, Singh J, Salto IP, Steiner ST, Kirse TM, Niemann S, Strassert CA, Faust A. Conjugated Pt(II) Complexes as Luminescence-Switch-On Reporters Addressing the Microenvironment of Bacterial Biofilms. Inorg Chem 2021: epub. Abstract

    2020

    Backhaus P, Roll W, Beuker C, Zinnhardt B, Seifert R, Wenning C, Eisenblatter M, Thomas C, Schmidt-Pogoda A, Strunk D, Wagner S, Faust A, Tuttelmann F, Ropke A, Jacobs AH, Stummer W, Wiendl H, Meuth SG, Schafers M, Grauer O, Minnerup J. Initial experience with [(18)F]DPA-714 TSPO-PET to image inflammation in primary angiitis of the central nervous system. Eur J Nucl Med Mol Imaging 2020Abstract
    Erdeljac N, Thiehoff C, Jumde RP, Daniliuc CG, Hoppner S, Faust A, Hirsch AKH, Gilmour R. Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF3 and Et Using Matrix Metalloproteinases As Structural Probes. J Med Chem 2020;63: 6225-6237. Abstract
    Sidharth TS, Maisuls I, Kösters J, Hepp A, Faust A, Voskuhl J, Strassert CA. Naphthalonitriles featuring efficient emission in solution and in the solid state. Beilstein J. Org. Chem. 2020;16: 2960-2970. Abstract

    2018

    Axer A, Hermann S, Kehr G, Clases D, Karst U, Fischer-Riepe L, Roth J, Fobker M, Schafers M, Gilmour R, Faust A. Harnessing the Maltodextrin Transport Mechanism for Targeted Bacterial Imaging: Structural Requirements for Improved in vivo Stability in Tracer Design. ChemMedChem 2018;13: 241-250. Abstract
    Delcanale P, Galstyan A, Daniliuc CG, Grecco HE, Abbruzzetti S, Faust A, Viappiani C, Strassert CA. Oxygen-Insensitive Aggregates of Pt(II) Complexes as Phosphorescent Labels of Proteins with Luminescence Lifetime-Based Readouts. ACS Appl Mater Interfaces 2018;10: 24361-24369. Abstract
    Duffy MJ, Planas O, Faust A, Vogl T, Hermann S, Schäfers M, Nonell S, Strassert CA. Towards optimized naphthalocyanines as sonochromes for photoacoustic imaging in vivo. Photoacoustics 2018;9: 49-61. Abstract
    Gruner MC, Niemann S, Faust A, Strassert CA. Axially Decorated Si(IV) -phthalocyanines Bearing Mannose- or Ammonium-conjugated Siloxanes: Comparative Bacterial Labeling and Photodynamic Inactivation. Photochem Photobiol 2018;94: 890-899. Abstract
    Neumann P-A, Twardy V, Becker F, Geyer C, Schwegmann K, Mohr A, Faust A, Lenz P, Rijcken E. Assessment of MMP-2/-9 expression by fluorescence endoscopy for evaluation of anastomotic healing in a murine model of anastomotic leakage. PLoS One 2018;13: e0194249. Abstract
    Voeller T, Faust A, Roth J, Schafers M, Vogl T, Hermann S. A Non-Peptidic S100A9 Specific Ligand for Optical Imaging of Phagocyte Activity In Vivo. Mol Imaging Biol 2018;20: 407-416. Abstract

    2017

    Clases D, Birka M, Sperling M, Faust A, Karst U. Isobaric dilution analysis as a calibration tool for long lived radionuclides in ICP-MS. J Trace Elem Med Biol 2017;40: 97-103. Abstract
    Höltke C, Faust A. Molecular imaging of integrins in oncology. Rmi 2017;Volume 10: 17-30. Abstract
    Zinnhardt B, Pigeon H, Theze B, Viel T, Wachsmuth L, Fricke IB, Schelhaas S, Honold L, Schwegmann K, Wagner S, Faust A, Faber C, Kuhlmann MT, Hermann S, Schafers M, Winkeler A, Jacobs AH. Combined PET Imaging of the Inflammatory Tumor Microenvironment Identifies Margins of Unique Radiotracer Uptake. Cancer Res 2017;77: 1831-1841. Abstract

    2016

    Bettenworth D, Mucke MM, Schwegmann K, Faust A, Poremba C, Schafers M, Domagk D, Lenz P. Endoscopy-guided orthotopic implantation of colorectal cancer cells results in metastatic colorectal cancer in mice. Clin Exp Metastasis 2016;33: 551-562. Abstract
    Faust A, Hermann S, Schafers M, Holtke C. Optical imaging probes and their potential contribution to radiotracer development. Nuklearmedizin 2016;55: 51-62. Abstract
    Fricke IB, Viel T, Worlitzer MM, Collmann FM, Vrachimis A, Faust A, Wachsmuth L, Faber C, Dolle F, Kuhlmann MT, Schafers K, Hermann S, Schwamborn JC, Jacobs AH. 6-hydroxydopamine-induced Parkinson's disease-like degeneration generates acute microgliosis and astrogliosis in the nigrostriatal system but no bioluminescence imaging-detectable alteration in adult neurogenesis. Eur J Neurosci 2016;43: 1352-1365. Abstract
    Galstyan A, Block D, Niemann S, Gruner MC, Abbruzzetti S, Oneto M, Daniliuc CG, Hermann S, Viappiani C, Schafers M, Loffler B, Strassert CA, Faust A. Corrigendum: Labeling and Selective Inactivation of Gram-Positive Bacteria Employing Bimodal Photoprobes with Dual Readouts. Chemistry 2016;22: 9051. Abstract
    Galstyan A, Block D, Niemann S, Gruner MC, Abbruzzetti S, Oneto M, Daniliuc CG, Hermann S, Viappiani C, Schafers M, Loffler B, Strassert CA, Faust A. Labeling and Selective Inactivation of Gram-Positive Bacteria Employing Bimodal Photoprobes with Dual Readouts. Chemistry 2016;22: 5243-5252. Abstract
    Galstyan A, Riehemann K, Schäfers M, Faust A. A combined experimental and computational study of the substituent effect on the photodynamic efficacy of amphiphilic Zn(ii)phthalocyanines. J. Mater. Chem. B 2016;4: 5683-5691. Abstract
    Gerwien H, Hermann S, Zhang X, Korpos E, Song J, Kopka K, Faust A, Wenning C, Gross CC, Honold L, Melzer N, Opdenakker G, Wiendl H, Schafers M, Sorokin L. Imaging matrix metalloproteinase activity in multiple sclerosis as a specific marker of leukocyte penetration of the blood-brain barrier. Sci Transl Med 2016;8: 364ra152. Abstract
    Schwegmann K, Bettenworth D, Hermann S, Faust A, Poremba C, Foell D, Schafers M, Domagk D, Lenz P. Detection of Early Murine Colorectal Cancer by MMP-2/-9-Guided Fluorescence Endoscopy. Inflamm Bowel Dis 2016;22: 82-91. Abstract
    Vrachimis A, Honold L, Faust A, Hermann S, Schafers M. New molecular probes of vascular inflammation. Q J Nucl Med Mol Imaging 2016;60: 194-204. Abstract

    2015

    Faust A, Voller T, Busch F, Schafers M, Roth J, Hermann S, Vogl T. Development and evaluation of a non-peptidic ligand for the molecular imaging of inflammatory processes using S100A9 (MRP14) as a novel target. Chem Commun (Camb) 2015;51: 15637-15640. Abstract
    Junker A, Kokornaczyk AK, Zweemer AJM, Frehland B, Schepmann D, Yamaguchi J, Itami K, Faust A, Hermann S, Wagner S, Schafers M, Koch M, Weiss C, Heitman LH, Kopka K, Wunsch B. Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists. Org Biomol Chem 2015;13: 2407-2422. Abstract
    Waldmann CM, Hermann S, Faust A, Riemann B, Schober O, Schafers M, Haufe G, Kopka K. Novel fluorine-18 labeled 5-(1-pyrrolidinylsulfonyl)-7-azaisatin derivatives as potential PET tracers for in vivo imaging of activated caspases in apoptosis. Bioorg Med Chem 2015;23: 5734-5739. Abstract
    Zinnhardt B, Viel T, Wachsmuth L, Vrachimis A, Wagner S, Breyholz H-J, Faust A, Hermann S, Kopka K, Faber C, Dolle F, Pappata S, Planas AM, Tavitian B, Schafers M, Sorokin LM, Kuhlmann MT, Jacobs AH. Multimodal imaging reveals temporal and spatial microglia and matrix metalloproteinase activity after experimental stroke. J Cereb Blood Flow Metab 2015;35: 1711-1721. Abstract

    2014

    Junker A, Schepmann D, Yamaguchi J, Itami K, Faust A, Kopka K, Wagner S, Wünsch B. Diverse modifications of the 4-methylphenyl moiety of TAK-779 by late-stage Suzuki-Miyaura cross-coupling. Org Biomol Chem 2014;12: 177-186. Abstract
    Vogl T, Eisenblatter M, Voller T, Zenker S, Hermann S, van Lent P, Faust A, Geyer C, Petersen B, Roebrock K, Schafers M, Bremer C, Roth J. Alarmin S100A8/S100A9 as a biomarker for molecular imaging of local inflammatory activity. Nat Commun 2014;5: 4593. Abstract

    2013

    Steingräber AK, Schelhaas S, Faust A, Jacobs AH, Schäfers M, Goerge T. Molecular imaging reveals time course of MMP activity in acute cutaneous vasculitis in vivo. Exp Dermatol 2013;22: 730-735. Abstract
    Waerzeggers Y, Viel T, Schäfers S, Wagner S, Faust A, Riemann B, Kopka K, Schober O, Schäfers K, Jacobs AH. Positron Emission Tomography (PET)-based Molecular Imaging. Part 5 - Imaging Technologies in Animal Tumor Models: Measuring Brain Tumor Growth and Metabolism 2013;Neuromethods; 77: 301-327.
    Waschkau B, Faust A, Schäfers M, Bremer C. Performance of a new fluorescence-labeled MMP inhibitor to image tumor MMP activity in vivo in comparison to an MMP-activatable probe. Contrast Media Mol Imaging 2013;8: 1-11. Abstract

    2012

    Claesener M, Breyholz H-J, Hermann S, Faust A, Wagner S, Schober O, Schäfers M, Kopka K. Efficient synthesis of a fluorine-18 labeled biotin derivative. Nucl Med Biol 2012;39: 1189-1194. Abstract

    2011

    Baumann A, Faust A, Law MP, Kuhlmann MT, Kopka K, Schäfers M, Karst U. Metabolite identification of a radiotracer by electrochemistry coupled to liquid chromatography with mass spectrometric and radioactivity detection. Anal Chem 2011;83: 5415-5421. Abstract
    Waerzeggers Y, Monfared P, Viel T, Faust A, Kopka K, Schäfers M, Tavitian B, Winkeler A, Jacobs A. Specific biomarkers of receptors, pathways of inhibition and targeted therapies: pre-clinical developments. Br J Radiol 2011;84 Spec No 2: S168-78. Abstract
    Wagner S, Faust A, Breyholz H-J, Schober O, Schäfers M, Kopka K. The MMP inhibitor (R)-2-(N-benzyl-4-(2-[18F]fluoroethoxy)phenylsulphonamido)-N-hydroxy-3-met hylbutanamide: Improved precursor synthesis and fully automated radiosynthesis. Appl Radiat Isot 2011;69: 862-868. Abstract
    Wagner S, Hugenberg V, Breyholz HJ, Faust A, Schober O, Schäfers M, Kopka K. Highly potent matrix metalloproteinase inhibitors based on triazole-substituted hydroxamic acids: synthesis, in vitro evaluation and 18F-radiolabelling. J Label Compd Radiopharm 2011;54: 150.

    2010

    Breyholz HJ, Wagner S, Faust A, Riemann B, Höltke C, Hermann S, Schober O, Schäfers M, Kopka K. Radiofluorinated pyrimidine-2,4,6-triones as molecular probes for noninvasive MMP-targeted imaging. ChemMedChem 2010;5: 777-789. Abstract

    2009

    Faust A, Hermann S, Wagner S, Haufe G, Schober O, Schäfers M, Kopka K. Molecular imaging of apoptosis in vivo with scintigraphic and optical biomarkers - a status report. Anticancer Agents Med Chem 2009;9: 968-985. Abstract
    Faust A, Waschkau B, Waldeck J, Höltke C, Breyholz H-J, Wagner S, Kopka K, Schober O, Heindel W, Schäfers M, Bremer C. Synthesis and evaluation of a novel hydroxamate based fluorescent photoprobe for imaging of matrix metalloproteinases. Bioconjug Chem 2009;20: 904-912. Abstract
    Höltke C, Faust A, Breyholz H-J, Kopka K, Schober O, Riemann B, Bremer C, Schäfers M, Wagner S. Non-invasive approaches to visualize the endothelin axis in vivo using state-of-the-art molecular imaging modalities. Mini Rev Med Chem 2009;9: 1580-1595. Abstract
    Höltke C, Law MP, Wagner S, Kopka K, Faust A, Breyholz H-J, Schober O, Bremer C, Riemann B, Schäfers M. PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies. Bioorg Med Chem 2009;17: 7197-7208. Abstract
    Kopka K, Faust A, Hermann S, Kuhlmann M, Wagner S, Klohs J, Schober O, Wunder A, Schäfers M. 18F-Labeled Isatin as putative biomarker for the specific imaging of activated caspases in apoptosis. J Labelled Comp Radiopharm 2009;52: S39-S39.
    Podichetty AK, Faust A, Kopka K, Wagner S, Schober O, Schäfers M, Haufe G. Fluorinated isatin derivatives Part 1: synthesis of new N-substituted (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatins as potent caspase-3 and -7 inhibitors. Bioorg Med Chem 2009;17: 2680-2688. Abstract
    Podichetty AK, Wagner S, Faust A, Schäfers M, Schober O, Kopka K, Haufe G. Fluorinated isatin derivatives Part 3 New side-chain fluoro-functionalized pyrrolidinyl sulfonyl isatins as potent caspase-3 and -7 inhibitors. Future Med Chem 2009;1: 969-989. Abstract
    Podichetty AK, Wagner S, Kopka K, Schröer S Faust A Schäfers M, Schober O, Haufe G. New N-Substituted 5-Pyrrolidinylsulfonyl Isatins as Potential Tools for Imaging of Caspases in Apoptosis by Positron Emission Tomography. J Med Chem 2009;52: 3484-3495.
    Podichetty AK, Wagner S, Schroer S, Faust A, Schäfers M, Schober O, Kopka K, Haufe G. Fluorinated isatin derivatives Part 2 New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis. J.Med.Chem. 2009;52: 3484-3495. Abstract
    Wagner S, Breyholz H-J, Höltke C, Faust A, Schober O, Schäfers M, Kopka K. A new 18F-labelled derivative of the MMP inhibitor CGS 27023A for PET: radiosynthesis and initial small-animal PET studies. Appl Radiat Isot 2009;67: 606-610. Abstract

    2008

    Faust A, Waschkau B, Waldeck J, Höltke C, Breyholz H-J, Wagner S, Kopka K, Heindel W, Schäfers M, Bremer C. Synthesis and evaluation of a novel fluorescent photoprobe for imaging matrix metalloproteinases. Bioconjug Chem 2008;19: 1001-1008. Abstract
    Kopka K, Hermann S, Faust A, Kuhlmann M, Wagner S, Breyholz HJ, Schober O, Schäfers M. Imaging of the "roads to ruin": 18F-labelled isatin as potential tracer for the molecular visualisation of activated caspases in apoptosis. Q J Nucl Med Mol Imaging 2008;52: 21-22.

    2007

    Faust A, Wagner S, Law MP, Hermann S, Schnöckel U, Keul P, Schober O, Schäfers M, Levkau B, Kopka K. The nonpeptidyl caspase binding radioligand (S)-1-(4-(2-[18F]Fluoroethoxy)-benzyl)-5-[1-(2-methoxymethylpyrrolidinyl)s ulfonyl]isatin ([18F]CbR) as potential positron emission tomography-compatible apoptosis imaging agent. Q J Nucl Med Mol Imaging 2007;51: 67-73. Abstract
    Höltke C, Wagner S, Breyholz HJ, Faust A, Law MP, Schäfers M, Kopka K. Developement, synthesis and in vitro evaluation of novel et-a receptor pet-radioligands based on pd 156707. J Labelled Comp Radiopharm 2007;50: 258.
    Wagner S, Breyholz H-J, Law MP, Faust A, Höltke C, Schroer S, Haufe G, Levkau B, Schober O, Schäfers M, Kopka K. Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET. J Med Chem 2007;50: 5752-5764. Abstract
    Wagner S, Breyholz HJ, Law MP, Faust A, Hoeltke C, Schober O, Schäfers M, Kopka K. Fluorinated derivatives of the potent matrix metalloproteinase inhibitors CGS 25966 and CGS 27023A: (Radio)syntheses and in vitro evaluation. J Label Compd Radiopharm 2007;50: 62.

    2006

    Kopka K, Faust A, Keul P, Wagner S, Breyholz H-J, Höltke C, Schober O, Schäfers M, Levkau B. 5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis. J Med Chem 2006;49: 6704-6715. Abstract
    Wagner S, Breyholz H-J, Faust A, Holtke C, Levkau B, Schober O, Schafers M, Kopka K. Molecular imaging of matrix metalloproteinases in vivo using small molecule inhibitors for SPECT and PET. Curr Med Chem 2006;13: 2819-2838. Abstract
    Wagner S, Law MP, Riemann B, Pike VW, Breyholz H-J, Höltke C, Faust A, Renner C, Schober O, Schäfers M, Kopka K. Synthesis of an 18F-labelled high affinity β1-adrenoceptor PET radioligand based on ICI 89,406. J Label Compd Radiopharm 2006;49: 177-195. Abstract

    2005

    Breyholz HJ, Schäfers M, Wagner S, Höltke C, Faust A, Rabeneck H, Levkau B, Schober O, Kopka K. C-5-disubstituted barbiturates as potential molecular probes for noninvasive matrix metalloproteinase imaging. J Med Chem 2005;48: 3400-3409. Abstract
    Wagner S, Law MP, Riemann B, Pike VW, Breyholz H-J, Höltke C, Faust A, Schober O, Schäfers M, Kopka K. Synthesis of (R)- and (S)-[O-methyl-11C]N-[2-[3-(2-cyano-phenoxy)-2-hydroxy-propylamino]-ethyl]-N′-(4-methoxy-phenyl)-urea as candidate high affinity β1-adrenoceptor PET radioligands. J Label Compd Radiopharm 2005;48: 721-733. Abstract

  • Patents

    Faust A, Hermann S, Roth J, Schäfers M, Vogl T. Quinolone-3-carboxamide compounds and their use in diagnosis. WO 2016067238 A1; publication date: 06/05/2016. PCT/IB2015/058348; publication date: 06/05/2016.

    Chen G, Gangadharmath UB, Kasi D, Kolb HC, Liu C, Sinha A, Szardenings AK, Walsh JC, Wang E, Yu C, Zhang W, Kopka K, Haufe G, Schäfers M, Hugenberg V, Wagner S, Hermann S, Breyholz H-J, Faust A. Compounds with matrix-metalloproteinase inhibitory activity and imaging agents thereof. EP 2644601; 02/10/2013.