Decisive role of water and protein dynamics in residence time of p38α MAP kinase inhibitors

por Pantsar, Tatu, Kaiser, Philipp D., Kudolo, Mark, Forster, Michael, Rothbauer, Ulrich, Laufer, Stefan A.
Publicado 2022

From 2-Alkylsulfanylimidazoles to 2-Alkylimidazoles: An Approach towards Metabolically More Stable p38α MAP Kinase Inhibitors

por Heider, Fabian, Haun, Urs, Döring, Eva, Kudolo, Mark, Sessler, Catharina, Albrecht, Wolfgang, Laufer, Stefan, Koch, Pierre
Publicado 2017

Design, Synthesis and Biological Evaluation of 7-Chloro-9H-pyrimido[4,5-b]indole-based Glycogen Synthase Kinase-3β Inhibitors

por Andreev, Stanislav, Pantsar, Tatu, Ansideri, Francesco, Kudolo, Mark, Forster, Michael, Schollmeyer, Dieter, Laufer, Stefan A., Koch, Pierre
Publicado 2019

Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2)

por Gerstenecker, Stefan, Haarer, Lisa, Schröder, Martin, Kudolo, Mark, Schwalm, Martin P., Wydra, Valentin, Serafim, Ricardo A. M., Chaikuad, Apirat, Knapp, Stefan, Laufer, Stefan, Gehringer, Matthias
Publicado 2021

Structural Optimization of a Pyridinylimidazole Scaffold: Shifting the Selectivity from p38α Mitogen-Activated Protein Kinase to c-Jun N-Terminal Kinase 3

por Ansideri, Francesco, Macedo, Joana T., Eitel, Michael, El-Gokha, Ahmed, Zinad, Dhafer S., Scarpellini, Camilla, Kudolo, Mark, Schollmeyer, Dieter, Boeckler, Frank M., Blaum, Bärbel S., Laufer, Stefan A., Koch, Pierre
Publicado 2018

Discovery and Evaluation of Enantiopure 9H-pyrimido[4,5-b]indoles as Nanomolar GSK-3β Inhibitors with Improved Metabolic Stability

por Andreev, Stanislav, Pantsar, Tatu, El-Gokha, Ahmed, Ansideri, Francesco, Kudolo, Mark, Anton, Débora Bublitz, Sita, Giulia, Romasco, Jenny, Geibel, Christian, Lämmerhofer, Michael, Goettert, Márcia Ines, Tarozzi, Andrea, Laufer, Stefan A., Koch, Pierre
Publicado 2020