G
Grzegorz Dubin
Researcher at Jagiellonian University
Publications - 122
Citations - 4107
Grzegorz Dubin is an academic researcher from Jagiellonian University. The author has contributed to research in topics: Proteases & Protease. The author has an hindex of 30, co-authored 110 publications receiving 3154 citations. Previous affiliations of Grzegorz Dubin include Ruhr University Bochum & Max Planck Society.
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Journal ArticleDOI
Structure of the Complex of Human Programmed Death 1, PD-1, and Its Ligand PD-L1.
Krzysztof M. Zak,Radoslaw Kitel,Sara Przetocka,Przemyslaw Golik,Katarzyna Guzik,Bogdan Musielak,Alexander Dömling,Grzegorz Dubin,Tad A. Holak,Tad A. Holak +9 more
TL;DR: It is shown that the ligand binding to human PD-1 is associated with significant plasticity within the receptor, and a detailed molecular map of the interaction surface is provided, allowing definition of the regions within both interacting partners that may likely be targeted by small molecules.
Journal ArticleDOI
Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)
Krzysztof M. Zak,Przemyslaw Grudnik,Katarzyna Guzik,Bartosz J. Zieba,Bogdan Musielak,Alexander Dömling,Grzegorz Dubin,Tad A. Holak,Tad A. Holak +8 more
TL;DR: It is shown that these small-molecule compounds bind directly to PD-L1 and that they potently block PD-1 binding.
Journal ArticleDOI
Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2
Krzysztof M. Zak,Przemyslaw Grudnik,Katarzyna Magiera,Alexander Dömling,Grzegorz Dubin,Tad A. Holak,Tad A. Holak +6 more
TL;DR: The latest work on structural characterization of the checkpoint proteins, their interactions with cognate ligands and with therapeutic antibodies reveals that they all have a similar modular structure, composed of small domains similar in topology to the domains found in antibodies.
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Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1
Katarzyna Guzik,Krzysztof M. Zak,Przemyslaw Grudnik,Katarzyna Magiera,Bogdan Musielak,Ricarda Törner,Lukasz Skalniak,Alexander Dömling,Grzegorz Dubin,Tad A. Holak +9 more
TL;DR: NMR and X-ray characterization is presented for the two classes of small-molecule PD-1/PD-L1 inhibitors that carry a number of disadvantages such as the high cost of the antibodies, their limited half-life, and immunogenicity.
Journal ArticleDOI
Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells
Lukasz Skalniak,Krzysztof M. Zak,Katarzyna Guzik,Katarzyna Magiera,Bogdan Musielak,Magdalena Pachota,Bozena Szelazek,Justyna Kocik,Przemyslaw Grudnik,Marcin Tomala,Sylwia Krzanik,Krzysztof Pyrc,Alexander Dömling,Grzegorz Dubin,Tad A. Holak +14 more
TL;DR: Evidence is provided that small molecules are capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes and the X-ray structures of the complexes of B MS-1001 and BMS-1166 were determined, which revealed features that may be responsible for increased potency of the compounds compared to their predecessors.