Publications of Tad Holak

Musielak, B.; Janczyk, W.; Rodriguez, I.; Plewka, J.; Sala, D.; Magiera-Mularz, K.; Holak, T.: Competition NMR for Detection of Hit/Lead Inhibitors of Protein-Protein Interactions. Molecules 25 (13), 3017 (2020)

Konstantinidou, M.; Zarganes-Tzitzikas, T.; Magiera-Mularz, K.; Holak, T. A.; Domling, A.: Immune Checkpoint PD-1/PD-L1: Is There Life Beyond Antibodies? Angewandte Chemie International Edition 57 (18), pp. 4840 - 4848 (2018)

Magiera-Mularz, K.; Skalniak, L.; Zak, K. M.; Musielak, B.; Rudzinska-Szostak, E.; Berlicki, L.; Kocik, J.; Grudnik, P.; Sala, D.; Zarganes-Tzitzikas, T. et al.; Shaabani, S.; Doemling, A.; Dubin, G.; Holak, T. A.: Bioactive Macrocyclic Inhibitors of the PD-1/PD-L1 Immune Checkpoint. Angewandte Chemie International Edition 56 (44), pp. 13732 - 13735 (2017)

Twarda-Clapa, A.; Krzanik, S.; Kubica, K.; Guzik, K.; Labuzek, B.; Neochoritis, C. G.; Khoury, K.; Kowalska, K.; Czub, M.; Dubin, G. et al.; Domling, A.; Skalniak, L.; Holak, T. A.: 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. Journal of Medicinal Chemistry 60 (10), pp. 4234 - 4244 (2017)

Zak, K. M.; Grudnik, P.; Magiera, K.; Domling, A.; Dubin, G.; Holak, T. A.: Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2. Structure 25 (8), pp. 1163 - 1174 (2017)

Zak, K. M.; Grudnik, P.; Guzik, K.; Zieba, B. J.; Musielak, B.; Domling, A.; Dubin, G.; Holak, T. A.: Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1). Oncotarget 7 (21), pp. 30323 - 30335 (2016)

Ammon, T.; Mishra, S. K.; Kowalska, K.; Popowicz, G. M.; Holak, T. A.; Jentsch, S.: The conserved ubiquitin-like protein Hub1 plays a critical role in splicing in human cells. JOURNAL OF MOLECULAR CELL BIOLOGY 6 (4), pp. 312 - 323 (2014)

Boltjes, A.; Huang, Y.; van de Velde, R.; Rijkee, L.; Wolf, S.; Gaugler, J.; Lesniak, K.; Guzik, K.; Holak, T. A.; Dömling, A.: Fragment-Based Library Generation for the Discovery of a Peptidomimetic p53-Mdm4 Inhibitor. ACS COMBINATORIAL SCIENCE 16 (8), pp. 393 - 396 (2014)

Huang, Y.; Wolf, S.; Beck, B.; Koehler, L.-M.; Khoury, K.; Popowicz, G. M.; Goda, S. K.; Subklewe, M.; Twarda, A.; Holak, T. et al.; Domling, A.: Discovery of Highly Potent p53-MDM2 Antagonists and Structural Basis for Anti-Acute Myeloid Leukemia Activities. ACS CHEMICAL BIOLOGY 9 (3), pp. 802 - 811 (2014)

Peche, V. S.; Holak, T. A.; Burgute, B. D.; Kosmas, K.; Kale, S. P.; Wunderlich, F. T.; Elhamine, F.; Stehle, R.; Pfitzer, G.; Nohroudi, K. et al.; Addicks, K.; Stoeckigt, F.; Schrickel, J. W.; Gallinger, J.; Schleicher, M.; Noegel, A. A.: Ablation of cyclase-associated protein 2 (CAP2) leads to cardiomyopathy. CELLULAR AND MOLECULAR LIFE SCIENCES 70 (3), pp. 527 - 543 (2013)

Baek, S.; Kang, N. J.; Popowicz, G. M.; Arciniega Castro, M.; Jung, S. K.; Byun, S.; Song, N. R.; Heo, Y.-S.; Kim, B. Y.; Lee, H. J. et al.; Holak, T. A.; Augustin, M.; Bode, A. M.; Huber, R.; Dong, Z.; Lee, K. W.: Structural and Functional Analysis of the Natural JNK1 Inhibitor Quercetagetin. JOURNAL OF MOLECULAR BIOLOGY 425 (2), pp. 411 - 423 (2013)

Bista, M.; Wolf, S.; Khoury, K.; Kowalska, K.; Huang, Y.; Wrona, E.; Arciniega, M.; Popowicz, G. M.; Holak, T.; Domling, A.: Transient Protein States in Designing Inhibitors of the MDM2-p53 Interaction. STRUCTURE 21 (12), pp. 2143 - 2151 (2013)

Wang, W.; Cao, H.; Wolf, S.; Camacho-Horvitz, M. S.; Holak, T.; Domling, A.: Benzimidazole-2-one: A novel anchoring principle for antagonizing p53-Mdm2. BIOORGANIC & MEDICINAL CHEMISTRY 21 (14), pp. 3982 - 3995 (2013)

Koes, D.; Khoury, K.; Huang, Y. J.; Wang, W.; Bista, M.; Popowicz, G. M.; Wolf, S.; Holak, T. A.; Domling, A.; Camacho, C. J.: Enabling Large-Scale Design, Synthesis and Validation of Small Molecule Protein-Protein Antagonists. PLoS ONE 7 (3), e32839, pp. [1] - [8] (2012)

Baek, S.; Kutchukian, P. S.; Verdine, G. L.; Huber, R.; Holak, T. A.; Lee, K. W.; Popowicz, G. M.: Structure of the Stapled p53 Peptide Bound to Mdm2. Journal of the American Chemical Society 134 (1), pp. 103 - 106 (2012)

Huang, Y. J.; Wolf, S.; Koes, D.; Popowicz, G. M.; Camacho, C. J.; Holak, T. A.; Domling, A.: Exhaustive Fluorine Scanning toward Potent p53-Mdm2 Antagonists. ChemMedChem 7 (1), pp. 49 - 52 (2012)

Sitar, T.; Gallinger, J.; Ducka, A. M.; Ikonen, T. P.; Wohlhoefler, M.; Schmoller, K. M.; Bausch, A. R.; Joel, P.; Trybus, K. M.; Noegel, A. A. et al.; Schleicher, M.; Huber, R.; Holak, T. A.: Molecular architecture of the Spire-actin nucleus and its implication for actin filament assembly. Proceedings of the National Academy of Sciences of the United States of America 108 (49), pp. 19575 - 19580 (2011)

Graeber, M.; Janczyk, W.; Sperl, B.; Elumalai, N.; Kozany, C.; Hausch, F.; Holak, T. A.; Berg, T.: Selective Targeting of Disease-Relevant Protein Binding Domains by O-Phosphorylated Natural Product Derivatives. ACS Chemical Biology 6 (10), pp. 1008 - 1014 (2011)

Orth, M.; Mayer, B.; Rehm, K.; Rothweiler, U.; Heidmann, D.; Holak, T. A.; Stemmann, O.: Shugoshin is a Mad1/Cdc20-like interactor of Mad2. EMBO Journal 30 (14), pp. 2868 - 2880 (2011)

Mishra, S. K.; Ammon, T.; Popowicz, G. M.; Krajewski, M.; Nagel, R. J.; Ares, M.; Holak, T. A.; Jentsch, S.: Role of the ubiquitin-like protein Hub1 in splice-site usage and alternative splicing. Nature 474 (7350), pp. 173 - 178 (2011)