Browsing by Author "Kitel, Radoslaw"

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      Exploring the Surface of the Ectodomain of the PD-L1 Immune Checkpoint with Small-Molecule Fragments 

      Kitel, Radoslaw; Rodríguez Rodríguez, Ismael; Del Corte Solaguren-Beascoa, Xabier; Atmaj, Jack; Zarnik, Magdalena; Surmiak, Ewa; Muszak, Damian; Magiera-Mularz, Katarzyna; Popowicz, Grzegorz M.; Holak, Tad A.; Musielak, Bogdan (American Chemical Society, 2022-09-08)
      Development of small molecules targeting the PD-L1/PD-1 interface is advancing both in industry and academia, but only a few have reached early-stage clinical trials. Here, we take a closer look at the general druggability ...
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      Nutlin-3a-aa: Improving the Bioactivity of a p53/MDM2 Interaction Inhibitor by Introducing a Solvent-Exposed Methylene Group 

      Nietzold, Florian; Rubner, Stefan; Labuzek, Beata; Golik, Przemyslaw; Surmiak, Ewa; Del Corte Solaguren-Beascoa, Xabier; Kitel, Radoslaw; Protzel, Christoph; Reppich-Sacher, Regina; Stichel, Jan; Magiera-Mularz, Katarzyna; Holak, Tad A. A.; Berg, Thorsten (Wiley, 2023-03)
      Nutlin-3a is a reversible inhibitor of the p53/MDM2 interaction. We have synthesized the derivative Nutlin-3a-aa bearing an additional exocyclic methylene group in the piperazinone moiety. Nutlin-3a-aa is more active than ...