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Structure-affinity and structure-residence time relationships of macrocyclic Gα_q 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_q/11 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 ...