Picture of Anna Junker and another person working in the lab
© P. Dziemba

Receptor Ligands for Molecular Imaging Lab (Dr. Anna Junker, Emmy-Noether Junior Research Group Leader)

We design, synthesize and characterize pharmacologically novel receptor ligands for diagnostic and therapeutic applications in the fields of cancer, inflammation and neuropathic pain. We develop molecular imaging probes for studying biological processes in vitro and in vivo and combine the imaging probes with targeted-drug delivery approaches to enhance the effective concentration of the probe at the site of interest and hereby improve image contrast and therapeutic efficacy.

  • Projects

    Development of novel, subtype-specific HCN channel ligands

    Principal investigators: Anna Junker (EIMI)
    Project term: 10/2019 - 03/2024
    Project number: GRK2515/1 | DFG

    P2X7 and P2X4 Receptors in Cancer and Inflammation: Drug Development, Bioimaging, and Targeted Drug Delivery

    The P2X7 receptor (P2X7R) is emerging as a promising target for the treatment of breast cancer, pancreas cancer, and inflammatory diseases, whereas the P2X4 receptor (P2X4R) displays promising potential for the therapy of neuropathic pain. The proposed project aims to develop potent and selective P2X7R and P2X4R ligands as innovative drugs for bioimaging, and targeted drug delivery.

    Principal investigators: Anna Junker (EIMI)
    Project term: 05/2018 - 04/2023
    Project number: JU 2966/2-1 | DFG Emmy Noether-Programm

  • Team

     

  • Publications

    2023

    Patberg M, Oniani T, Disse P, Peischard S, Vinnenberg L, Zobeiri M, Romanelli MN, Epping L, Wiendl H, Meuth SG, Hundehege P, Seebohm G, Budde T, Junker A. Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18. Arch Pharm (Weinheim) 2023: e2200665. Abstract
    Schmidt S, Isaak A, Junker A. Spotlight on P2X7 Receptor PET Imaging: A Bright Target or a Failing Star?. Int J Mol Sci 2023;24Abstract

    2022

    Lemmerhirt JP, Isaak A, Liu R, Kock M, Daniliuc CG, Jacobson KA, Heitman LH, Junker A. Development of Bicyclo[310]hexane-Based A3 Receptor Ligands: Closing the Gaps in the Structure-Affinity Relationships. Molecules 2022;27Abstract
    Oniani T, Vinnenberg L, Chaudhary R, Schreiber JA, Riske K, Williams B, Pape H-C, White JA, Junker A, Seebohm G, Meuth SG, Hundehege P, Budde T, Zobeiri M. Effects of Axonal Demyelination, Inflammatory Cytokines and Divalent Cation Chelators on Thalamic HCN Channels and Oscillatory Bursting. Int J Mol Sci 2022;23Abstract
    Scortichini M, Idris RM, Moschutz S, Keim A, Salmaso V, Dobelmann C, Oliva P, Losenkova K, Irjala H, Vaittinen S, Sandholm J, Yegutkin GG, Strater N, Junker A, Muller CE, Jacobson KA. Structure-Activity Relationship of 3-Methylcytidine-5'-alpha,beta-methylenediphosphates as CD73 Inhibitors. J Med Chem 2022Abstract
    Turgutalp B, Bhattarai P, Ercetin T, Luise C, Reis R, Gurdal EE, Isaak A, Biriken D, Dinter E, Sipahi H, Schepmann D, Junker A, Wunsch B, Sippl W, Gulcan HO, Kizil C, Yarim M. Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease. J Med Chem 2022;65: 12292-12318. Abstract

    2021

    Oliva P, Scortichini M, Dobelmann C, Jain S, Gopinatth V, Toti KS, Phung NB, Junker A, Jacobson KA. Structure-activity relationships of pyrimidine nucleotides containing a 5'-alpha,beta-methylene diphosphonate at the P2Y6 receptor. Bioorg Med Chem Lett 2021;45: 128137. Abstract
    Patberg M, Isaak A, Fusser F, Ortiz Zacarias NV, Vinnenberg L, Schulte J, Michetti L, Grey L, van der Horst C, Hundehege P, Koch O, Heitman LH, Budde T, Junker A. Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists. Eur J Med Chem 2021;226: 113838. Abstract
    Silva DG, Feijens P-B, Hendrick R, Matheeussen A, Grey L, Caljon G, Maes L, Emery FS, Junker A. Development of Novel Isoindolone-Based Compounds against Trypanosoma brucei rhodesiense. ChemistryOpen 2021;10: 922-927. Abstract
    Silva DG, Junker A, de Melo SMG, Fumagalli F, Gillespie JR, Molasky N, Buckner FS, Matheeussen A, Caljon G, Maes L, Emery FS. Synthesis and Structure-Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases. ChemMedChem 2021;16: 966-975. Abstract
    Wagner S, de Moura Gatti F, Silva DG, Ortiz Zacarias NV, Zweemer AJM, Hermann S, De Maria M, Koch M, Weiss C, Schepmann D, Heitman LH, Tschammer N, Kopka K, Junker A. Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors. ChemMedChem 2021;16: 640-645. Abstract

    2019

    Junker A, Renn C, Dobelmann C, Namasivayam V, Jain S, Losenkova K, Irjala H, Duca S, Balasubramanian R, Chakraborty S, Börgel F, Zimmermann H, Yegutkin G G, Müller C E, Jacobson K A. Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors. J Med Chem 2019;11: 3677-3695. Abstract
    Liu Q, Junker A, Murakami K, Hu P. Automated Counting of Cancer Cells by Ensembling Deep Features. Cells 2019;8: 1019. Abstract

    2017

    Kokornaczyk AK, Thum S, Daniliuc CG, Junker A, Wünsch B. Molecular structure of a brominated 2-benzazepinone – a crucial intermediate in the synthesis of novel chemokine CCR2 receptor antagonists. Z. Naturforsch. B 2017;72: 421-424. Abstract
    Thum S, Kokornaczyk AK, Seki T, De Maria M, Ortiz Zacarias NV, de Vries H, Weiss C, Koch M, Schepmann D, Kitamura M, Tschammer N, Heitman LH, Junker A, Wunsch B. Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. Eur J Med Chem 2017;135: 401-413. Abstract

    2016

    Junker A, Balasubramanian R, Ciancetta A, Uliassi E, Kiselev E, Martiriggiano C, Trujillo K, Mtchedlidze G, Birdwell L, Brown KA, Harden TK, Jacobson KA. Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y(14) Receptor Antagonists. J. Med. Chem. 2016;59: 6149-6168. Abstract

    2015

    Junker A, Kokornaczyk AK, Strunz AK, Wünsch B. Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview. Top Med Chem 2015;14: 187-241. 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
    Strunz AK, Zweemer AJM, Weiss C, Schepmann D, Junker A, Heitman LH, Koch M, Wunsch B. Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). Bioorg Med Chem 2015;23: 4034-4049. Abstract

    2014

    Junker A, Kokornaczyk AK, Strunz AK, Wünsch B. Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview. Chemokines 2014: 1-55. Abstract
    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

    2013

    Junker A, Yamaguchi J, Itami K, Wunsch B. Synthesis of thiophene-based TAK-779 analogues by C-H arylation. J Org Chem 2013;78: 5579-5586. Abstract

  • Patents

    Junker A. Purine and Pyrimidine Nucleotides as Ecto-5’-Nucleotidase Inhibitors. U.S. Patent Application No. 62/719,492 filed August 17, 2018. HHS E-132-2018-0-US-01.

    Junker A. Triazole derivatives as P2Y14 receptor antagonists. U.S. Patent application No. US 62/233,162 filed September 25, 2015; filed as PCT on September 26, 2016 HHS E-213-2015/0-PCT-02; Issued on March 30th 2017, WO/2017/053769.