Home » Graduate Program (2018-2022) » Publications » Project 2

Validation of xenosensing nuclear receptor PXR as a therapeutic target in cancer chemotherapy

10 project-relevant publications [ICEPHA PI(s) and PhD student(s) in bold letters] 

  1. Abdelmalek CM, Hu Z, Kronenberger T, Kublbeck J, Kinnen FJM, Hesse SS, Malik A, Kudolo M, Niess R, Gehringer M, Zender L, Witt-Enderby PA, Zlotos DP, Laufer SA. 2022. Gefitinib-Tamoxifen Hybrid Ligands as Potent Agents against Triple-Negative Breast Cancer. J Med Chem 65:4616-32. doi:10.1021/acs.jmedchem.1c01646
  2. Burk O, Kronenberger T, Keminer O, Lee SML, Schiergens TS, Schwab M, Windshugel B. 2021. Nelfinavir and Its Active Metabolite M8 Are Partial Agonists and Competitive Antagonists of the Human Pregnane X Receptor. Mol Pharmacol 99:184-96. doi:10.1124/molpharm.120.000116
  3. Juchum M, Pfaffenrot B, Klovekorn P, Selig R, Albrecht W, Zender L, Laufer SA. 2022. Scaffold modified Vemurafenib analogues as highly selective mitogen activated protein kinase kinase 4 (MKK4) inhibitors. Eur J Med Chem 240:114584. doi:10.1016/j.ejmech.2022.114584
  4. Keminer O, Windshugel B, Essmann F, Lee SML, Schiergens TS, Schwab M, Burk O. 2019. Identification of novel agonists by high-throughput screening and molecular modelling of human constitutive androstane receptor isoform 3. Arch Toxicol 93:2247-64. doi:10.1007/s00204-019-02495-6
  5. Kircher T, Pantsar T, Oder A, Peter von Kries J, Juchum M, Pfaffenrot B, Kloevekorn P, Albrecht W, Selig R, Laufer S. 2021. Design and synthesis of novel fluorescently labeled analogs of vemurafenib targeting MKK4. Eur J Med Chem 209:112901. doi:10.1016/j.ejmech.2020.112901
  6. Mustonen EK, Pantsar T, Rashidian A, Reiner J, Schwab M, Laufer S, Burk O. 2022. Target Hopping from Protein Kinases to PXR: Identification of Small-Molecule Protein Kinase Inhibitors as Selective Modulators of Pregnane X Receptor from TuKIC Library. Cells 11:doi:10.3390/cells11081299
  7. Pantsar T, Kaiser PD, Kudolo M, Forster M, Rothbauer U, Laufer SA. 2022. Decisive role of water and protein dynamics in residence time of p38alpha MAP kinase inhibitors. Nat Commun 13:569. doi:10.1038/s41467-022-28164-4
  8. Pfaffenrot B, Klovekorn P, Juchum M, Selig R, Albrecht W, Zender L, Laufer SA. 2021. Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration. Eur J Med Chem 218:113371. doi:10.1016/j.ejmech.2021.
    113371
  9. Rudalska R, Harbig J, Snaebjornsson MT, Klotz S, Zwirner S, Taranets L, Heinzmann F, Kronenberger T, Forster M, Cui W, D'Artista L, Einig E, Hinterleitner M, Schmitz W, Dylawerska A, Kang TW, Poso A, Rosenfeldt MT, Malek NP, Bitzer M, Laufer S, Pichler BJ, Popov N, Schulze A, Zender L, Dauch D. 2021. LXRalpha activation and Raf inhibition trigger lethal lipotoxicity in liver cancer. Nat Cancer 2:201-17. doi:10.1038/s43018-020-00168-3
  10. Wittlinger F, Heppner DE, To C, Gunther M, Shin BH, Rana JK, Schmoker AM, Beyett TS, Berger LM, Berger BT, Bauer N, Vasta JD, Corona CR, Robers MB, Knapp S, Janne PA, Eck MJ, Laufer SA. 2022. Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. J Med Chem 65:1370-83. doi:10.1021/acs.jmedchem.1c00848