Pharmazeutisches Institut

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  • Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors 

    Voss, Jan H.; Crüsemann, Max; Bartling, Christian R.O.; Kehraus, Stefan; Inoue, Asuka; König, Gabriele M.; Strømgaard, Kristian; Müller, Christa E. (2023-04-21)
    The macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR) are potent inhibitors of Gα<sub>q/11</sub> proteins. They are important pharmacological tools and have potential as therapeutic drugs. The hydrogenated, ...

  • Mesoporous Silica as an Alternative Vehicle to Overcome Solubility Limitations 

    Becker, Tim; Heitkötter, Jan; Krome, Anna K.; Schiefer, Andrea; Pfarr, Kenneth; Ehrens, Alexandra; Grosse, Miriam; Sandargo, Birthe; Stammberger, Ingo; Stadler, Marc; Hübner, Marc P.; Kehraus, Stefan; Hoerauf, Achim; Wagner, Karl G. (2024-03-12)
    Toxicological studies are a part of the drug development process and the preclinical stages, for which suitable vehicles ensuring easy and safe administration are crucial. However, poor aqueous solubility of drugs complicates ...

  • Development of the first geldanamycin-based HSP90 degraders 

    Wurnig, Silas; Vogt, Melina; Hogenkamp, Julian; Dienstbier, Niklas; Borkhardt, Arndt; Bhatia, Sanil; Hansen, Finn (2023-06-28)
    Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting ...

  • A Systematic Database Approach to Identify Companion Diagnostic Testing in Clinical Trials under the New In Vitro Diagnostic Medical Devices Regulation 

    Wollenhaupt, Clara; Sudhop, Thomas; Knoess, Werner (2023-06-12)
    The European Union In Vitro Diagnostic Medical Devices Regulation (EU) 2017/746 (IVDR) introduces companion diagnostics (CDx) as a new legal term. CDx are applied in combination with a medicinal product to identify patient ...

  • Irreversible Antagonists for the Adenosine A2B Receptor 

    Temirak, Ahmed; Schlegel, Jonathan; Voss, Jan; Vaaßen, Victoria; Vielmuth, Christin; Claff, Tobias; Müller, Christa (2022-06-13)
    Blockade of the adenosine A2B receptor (A2BAR) represents a potential novel strategy for the immunotherapy of cancer. In the present study, we designed, synthesized, and characterized irreversible A2BAR antagonists based ...