Radosław Nowak's Publications
Our latest publications can always be found on Google Scholar.
2023
Zou, C.; Yoon, H.; Park, P. M. C.; Patten, J. J.; Pellman, J.; Carreiro, J.; Tsai, J. M.; Li, Y. D.; Roy Burman, S. S.; Donovan, K. A.; Gasser, J.; Sperling, A. S.; Nowak, R. P.; Fischer, E. S.; Davey, R. A.; Ebert, B. L.; Slabicki, M. The human E3 ligase RNF185 is a regulator of the SARS-CoV-2 envelope protein. iScience 2023, 26 (5), 106601. DOI: 10.1016/j.isci.2023.106601.
Yue, H.; Nowak, R. P.; Overwijn, D.; Payne, N. C.; Fischinger, S.; Atyeo, C.; Lam, E. C.; St Denis, K.; Brais, L. K.; Konishi, Y.; Sklavenitis-Pistofidis, R.; Baden, L. R.; Nilles, E. J.; Karlson, E. W.; Yu, X. G.; Li, J. Z.; Woolley, A. E.; Ghobrial, I. M.; Meyerhardt, J. A.; Balazs, A. B.; Alter, G.; Mazitschek, R.; Fischer, E. S. Diagnostic TR-FRET assays for detection of antibodies in patient samples. Cell Rep Methods 2023, 3 (3), 100421. DOI: 10.1016/j.crmeth.2023.100421 From NLM Medline.
Nowak, R. P.; Che, J.; Ferrao, S.; Kong, N. R.; Liu, H.; Zerfas, B. L.; Jones, L. H. Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives. RSC Med Chem 2023, 14 (3), 501-506. DOI: 10.1039/d2md00347c From NLM PubMed-not-MEDLINE.
Perner, F.; Stein, E. M.; Wenge, D. V.; Singh, S.; Kim, J.; Apazidis, A.; Rahnamoun, H.; Anand, D.; Marinaccio, C.; Hatton, C.; Wen, Y.; Stone, R. M.; Schaller, D.; Mowla, S.; Xiao, W.; Gamlen, H. A.; Stonestrom, A. J.; Persaud, S.; Ener, E.; Cutler, J. A.; Doench, J. G.; McGeehan, G. M.; Volkamer, A.; Chodera, J. D.; Nowak, R. P.; Fischer, E. S.; Levine, R. L.; Armstrong, S. A.; Cai, S. F. MEN1 mutations mediate clinical resistance to menin inhibition. Nature 2023. DOI: 10.1038/s41586-023-05755-9.
Teng, M.; Jiang, J.; Wang, E. S.; Geng, Q.; Toenjes, S. T.; Donovan, K. A.; Mageed, N.; Yue, H.; Nowak, R. P.; Wang, J.; Manz, T. D.; Fischer, E. S.; Cantley, L. C.; Gray, N. S. Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader. Angew Chem Int Ed Engl 2023, e202302364. DOI: 10.1002/anie.202302364.
Hanzl, A.; Barone, E.; Bauer, S.; Yue, H.; Nowak, R. P.; Hahn, E.; Pankevich, E. V.; Koren, A.; Kubicek, S.; Fischer, E. S.; Winter, G. E. E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance. J Am Chem Soc 2023, 145 (2), 1176-1184. DOI: 10.1021/jacs.2c10784.
Li, J.; Wang, L.; Hahn, Q.; Nowak, R. P.; Viennet, T.; Orellana, E. A.; Roy Burman, S. S.; Yue, H.; Hunkeler, M.; Fontana, P.; Wu, H.; Arthanari, H.; Fischer, E. S.; Gregory, R. I. Structural basis of regulated m(7)G tRNA modification by METTL1-WDR4. Nature 2023, 613 (7943), 391-397. DOI: 10.1038/s41586-022-05566-4.
Boytz, R.; Slabicki, M.; Ramaswamy, S.; Patten, J. J.; Zou, C.; Meng, C.; Hurst, B. L.; Wang, J.; Nowak, R. P.; Yang, P. L.; Sattler, M.; Stone, R. M.; Griffin, J. D.; Gray, N. S.; Gummuluru, S.; Davey, R. A.; Weisberg, E. Anti-SARS-CoV-2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID-19 therapy. J Med Virol 2023, 95 (1), e28157. DOI: 10.1002/jmv.28157.
Tsang, T.; Huerta, F.; Liu, Y.; Che, J.; Metivier, R. J.; Ferrao, S.; Donovan, K. A.; Jones, L. H.; Zerfas, B. L.; Nowak, R. P. HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development. ACS Chem Biol 2023, 18 (4), 933-941. DOI: 10.1021/acschembio.3c00084.
Gao, Y.; Jiang, B.; Kim, H.; Berberich, M. J.; Che, J.; Donovan, K. A.; Hatcher, J. M.; Huerta, F.; Kwiatkowski, N. P.; Liu, Y.; Liuni, P. P.; Metivier, R. J.; Murali, V. K.; Nowak, R. P.; Zhang, T.; Fischer, E. S.; Gray, N. S.; Jones, L. H. Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions. J Med Chem 2023. DOI: 10.1021/acs.jmedchem.2c01864.
Cruite, J. T.; Nowak, R. P.; Donovan, K. A.; Ficarro, S. B.; Huang, H.; Liu, H.; Liu, Y.; Marto, J. A.; Metivier, R. J.; Fischer, E. S.; Jones, L. H. Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange. ACS Medicinal Chemistry Letters 2023. DOI: 10.1021/acsmedchemlett.3c00371.
Nowak, R. P.; Ragosta, L.; Huerta, F.; Liu, H.; Ficarro, S. B.; Cruite, J. T.; Metivier, R. J.; Donovan, K. A.; Marto, J. A.; Fischer, E. S.; Zerfas, B. L.; Jones, L. H. Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead. RSC Chemical Biology 2023, 10.1039/D3CB00103B. DOI: 10.1039/D3CB00103B.
2022
Verano, A. L.; You, I.; Donovan, K. A.; Mageed, N.; Yue, H.; Nowak, R. P.; Fischer, E. S.; Wang, E. S.; Gray, N. S. Redirecting the Neo-Substrate Specificity of Cereblon-Targeting PROTACs to Helios. ACS Chem Biol 2022, 17 (9), 2404-2410. DOI: 10.1021/acschembio.2c00439.
Aubrey, B. J.; Cutler, J. A.; Bourgeois, W.; Donovan, K. A.; Gu, S.; Hatton, C.; Perlee, S.; Perner, F.; Rahnamoun, H.; Theall, A. C. P.; Henrich, J. A.; Zhu, Q.; Nowak, R. P.; Kim, Y. J.; Parvin, S.; Cremer, A.; Olsen, S. N.; Eleuteri, N. A.; Pikman, Y.; McGeehan, G. M.; Stegmaier, K.; Letai, A.; Fischer, E. S.; Liu, X. S.; Armstrong, S. A. IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia. Nat Cancer 2022, 3 (5), 595-613. DOI: 10.1038/s43018-022-00366-1.
Cruite, J. T.; Dann, G. P.; Che, J.; Donovan, K. A.; Ferrao, S.; Ficarro, S. B.; Fischer, E. S.; Gray, N. S.; Huerta, F.; Kong, N. R.; Liu, H.; Marto, J. A.; Metivier, R. J.; Nowak, R. P.; Zerfas, B. L.; Jones, L. H. Cereblon covalent modulation through structure-based design of histidine targeting chemical probes. RSC Chem Biol 2022, 3 (9), 1105-1110. DOI: 10.1039/d2cb00078d.
Du, G.; Jiang, J.; Henning, N. J.; Safaee, N.; Koide, E.; Nowak, R. P.; Donovan, K. A.; Yoon, H.; You, I.; Yue, H.; Eleuteri, N. A.; He, Z.; Li, Z.; Huang, H. T.; Che, J.; Nabet, B.; Zhang, T.; Fischer, E. S.; Gray, N. S. Exploring the target scope of KEAP1 E3 ligase-based PROTACs. Cell Chem Biol 2022. DOI: 10.1016/j.chembiol.2022.08.003.
Dann, G. P.; Liu, H.; Nowak, R. P.; Jones, L. H. Cereblon target validation using a covalent inhibitor of neosubstrate recruitment. In Methods in Enzymology, Academic Press, 2022.
Zerfas, B. L.; Huerta, F.; Liu, H.; Du, G.; Gray, N. S.; Jones, L. H.; Nowak, R. P. Advancing targeted protein degrader discovery by measuring cereblon engagement in cells. In Methods in Enzymology, Academic Press, 2022.
Meyerhardt, J. A.; Yue, H.; Nowak, R. P.; Brais, L.; Ma, C.; Johnson, S.; Harrod, J.; Burman, S. S. R.; Hendrickson, L. M.; Fischinger, S.; Alter, G.; Hahn, W.; Johnson, B. E.; Fischer, E. S. Serological testing for SARS-CoV-2 antibodies of employees shows low transmission working in a cancer center. PLoS One 2022, 17 (4), e0266791. DOI: 10.1371/journal.pone.0266791.
Silva, M. C.; Nandi, G.; Donovan, K. A.; Cai, Q.; Berry, B. C.; Nowak, R. P.; Fischer, E. S.; Gray, N. S.; Ferguson, F. M.; Haggarty, S. J. Discovery and Optimization of Tau Targeted Protein Degraders Enabled by Patient Induced Pluripotent Stem Cells-Derived Neuronal Models of Tauopathy. Front Cell Neurosci 2022, 16, 801179. DOI: 10.3389/fncel.2022.801179.
2021
Dubey, A.; Stoyanov, N.; Viennet, T.; Chhabra, S.; Elter, S.; Borggrafe, J.; Viegas, A.; Nowak, R. P.; Burdzhiev, N.; Petrov, O.; Fischer, E. S.; Etzkorn, M.; Gelev, V.; Arthanari, H. Local Deuteration Enables NMR Observation of Methyl Groups in Proteins from Eukaryotic and Cell-Free Expression Systems. Angew Chem Int Ed Engl 2021, 60 (25), 13783-13787. DOI: 10.1002/anie.202016070.
Wang, E. S.; Verano, A. L.; Nowak, R. P.; Yuan, J. C.; Donovan, K. A.; Eleuteri, N. A.; Yue, H.; Ngo, K. H.; Lizotte, P. H.; Gokhale, P. C.; Gray, N. S.; Fischer, E. S. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol 2021, 17 (6), 711-717. DOI: 10.1038/s41589-021-00802-w.
Xiong, Y.; Donovan, K. A.; Eleuteri, N. A.; Kirmani, N.; Yue, H.; Razov, A.; Krupnick, N. M.; Nowak, R. P.; Fischer, E. S. Chemo-proteomics exploration of HDAC degradability by small molecule degraders. Cell Chem Biol 2021. DOI: 10.1016/j.chembiol.2021.07.002.
Fischer, P. D.; Papadopoulos, E.; Dempersmier, J. M.; Wang, Z. F.; Nowak, R. P.; Donovan, K. A.; Kalabathula, J.; Gorgulla, C.; Junghanns, P. P. M.; Kabha, E.; Dimitrakakis, N.; Petrov, O. I.; Mitsiades, C.; Ducho, C.; Gelev, V.; Fischer, E. S.; Wagner, G.; Arthanari, H. A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders. Eur J Med Chem 2021, 219, 113435. DOI: 10.1016/j.ejmech.2021.113435.
Wright, N. D.; Collins, P.; Koekemoer, L.; Krojer, T.; Talon, R.; Nelson, E.; Ye, M.; Nowak, R.; Newman, J.; Ng, J. T.; Mitrovich, N.; Wiggers, H.; von Delft, F. The low-cost Shifter microscope stage transforms the speed and robustness of protein crystal harvesting. Acta Crystallogr D Struct Biol 2021, 77 (Pt 1), 62-74. DOI: 10.1107/S2059798320014114.
Teng, M.; Lu, W.; Donovan, K. A.; Sun, J.; Krupnick, N. M.; Nowak, R. P.; Li, Y. D.; Sperling, A. S.; Zhang, T.; Ebert, B. L.; Fischer, E. S.; Gray, N. S. Development of PDE6D and CK1alpha Degraders through Chemical Derivatization of FPFT-2216. J Med Chem 2021. DOI: 10.1021/acs.jmedchem.1c01832.
Wu, W.; Nelson, G.; Koch, R.; Donovan, K. A.; Nowak, R. P.; Heavican-Foral, T. B.; Nirmal, A. J.; Liu, H.; Yang, L.; Duffy, J.; Powers, F.; Stevenson, K. E.; Jones, M.; Ng, S. Y.; Wu, G.; Jain, S.; Xu, R.; Amaka, S.; Trevisani, C.; Donaldson, N.; Hagner, P. R.; de Leval, L.; Gaulard, P.; Iqbal, J.; Thakurta, A.; Fischer, E. S.; Adelman, K.; Weinstock, D. M. Overcoming IMiD Resistance in T-cell Lymphomas Through Potent Degradation of ZFP91 and IKZF1. Blood 2021. DOI: 10.1182/blood.2021014701.
Konishi, Y.; Sklavenitis-Pistofidis, R.; Yue, H.; Ferrari, F.; Redd, R. A.; Lightbody, E. D.; Russo, M.; Perry, J.; Horowitz, E.; Justis, A. V.; Shayegh, N. A.; Savell, A.; Prescott, J.; Varmeh, S.; Nowak, R. P.; Hamilton, M.; Auclair, D.; Marinac, C. R.; Trippa, L.; Fischer, E. S.; Ghobrial, I. M. Attenuated response to SARS-CoV-2 vaccine in patients with asymptomatic precursor stages of multiple myeloma and Waldenstrom macroglobulinemia. Cancer Cell 2021. DOI: 10.1016/j.ccell.2021.12.003.
Nowak, R. P.; Xiong, Y.; Kirmani, N.; Kalabathula, J.; Donovan, K. A.; Eleuteri, N. A.; Yuan, J. C.; Fischer, E. S. Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. J Med Chem 2021, 64 (15), 11637-11650. DOI: 10.1021/acs.jmedchem.1c00958.
Nowak, R. P.; Jones, L. H. Target Validation Using PROTACs: Applying the Four Pillars Framework. SLAS DISCOVERY: Advancing the Science of Drug Discovery 2021, 26 (4), 474-483.
Nowak, R. P.; Yue, H.; Park, E. Y.; Fischer, E. S. Methods for Quantitative Assessment of Protein Degradation. Methods Mol Biol 2021, 2365, 247-263. DOI: 10.1007/978-1-0716-1665-9_13.
2020
Powell, C. E.; Du, G.; Che, J.; He, Z.; Donovan, K. A.; Yue, H.; Wang, E. S.; Nowak, R. P.; Zhang, T.; Fischer, E. S.; Gray, N. S. Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. ACS Chem Biol 2020, 15 (10), 2722-2730. DOI: 10.1021/acschembio.0c00520.
Li, Z.; Pinch, B. J.; Olson, C. M.; Donovan, K. A.; Nowak, R. P.; Mills, C. E.; Scott, D. A.; Doctor, Z. M.; Eleuteri, N. A.; Chung, M.; Sorger, P. K.; Fischer, E. S.; Gray, N. S. Development and Characterization of a Wee1 Kinase Degrader. Cell Chem Biol 2020, 27 (1), 57-65 e59. DOI: 10.1016/j.chembiol.2019.10.013.
Zeng, M.; Xiong, Y.; Safaee, N.; Nowak, R. P.; Donovan, K. A.; Yuan, C. J.; Nabet, B.; Gero, T. W.; Feru, F.; Li, L.; Gondi, S.; Ombelets, L. J.; Quan, C.; Janne, P. A.; Kostic, M.; Scott, D. A.; Westover, K. D.; Fischer, E. S.; Gray, N. S. Exploring Targeted Degradation Strategy for Oncogenic KRAS(G12C). Cell Chem Biol 2020, 27 (1), 19-31 e16. DOI: 10.1016/j.chembiol.2019.12.006.
Faust, T. B.; Yoon, H.; Nowak, R. P.; Donovan, K. A.; Li, Z.; Cai, Q.; Eleuteri, N. A.; Zhang, T.; Gray, N. S.; Fischer, E. S. Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nat Chem Biol 2020, 16 (1), 7-14. DOI: 10.1038/s41589-019-0378-3.
Slabicki, M.; Yoon, H.; Koeppel, J.; Nitsch, L.; Roy Burman, S. S.; Di Genua, C.; Donovan, K. A.; Sperling, A. S.; Hunkeler, M.; Tsai, J. M.; Sharma, R.; Guirguis, A.; Zou, C.; Chudasama, P.; Gasser, J. A.; Miller, P. G.; Scholl, C.; Frohling, S.; Nowak, R. P.; Fischer, E. S.; Ebert, B. L. Small-molecule-induced polymerization triggers degradation of BCL6. Nature 2020, 588 (7836), 164-168. DOI: 10.1038/s41586-020-2925-1.
Jang, J.; To, C.; De Clercq, D. J. H.; Park, E.; Ponthier, C. M.; Shin, B. H.; Mushajiang, M.; Nowak, R. P.; Fischer, E. S.; Eck, M. J.; Janne, P. A.; Gray, N. S. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl 2020, 59 (34), 14481-14489. DOI: 10.1002/anie.202003500.
Morita, K.; He, S.; Nowak, R. P.; Wang, J.; Zimmerman, M. W.; Fu, C.; Durbin, A. D.; Martel, M. W.; Prutsch, N.; Gray, N. S.; Fischer, E. S.; Look, A. T. Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell 2020, 181 (3), 702-715 e720. DOI: 10.1016/j.cell.2020.03.051.
Gasic, I.; Groendyke, B. J.; Nowak, R. P.; Yuan, J. C.; Kalabathula, J.; Fischer, E. S.; Gray, N. S.; Mitchison, T. J. Tubulin Resists Degradation by Cereblon-Recruiting PROTACs. Cells 2020, 9 (5), 1083. DOI: 10.3390/cells9051083.
Yue, H.; Nowak, R. P.; Overwijn, D.; Payne, N. C.; Fischinger, S.; Atyeo, C.; Baden, L. R.; Nilles, E. J.; Karlson, E. W.; Xu, G. Y. Rapid'mix and read'assay for scalable detection of SARS-CoV-2 antibodies in patient plasma. medRxiv 2020.
Wu, T.; Yoon, H.; Xiong, Y.; Dixon-Clarke, S. E.; Nowak, R. P.; Fischer, E. S. Targeted protein degradation as a powerful research tool in basic biology and drug target discovery. Nature Structural & Molecular Biology 2020, 27 (7), 605-614.
2019
Dobrovolsky, D.; Wang, E. S.; Morrow, S.; Leahy, C.; Faust, T.; Nowak, R. P.; Donovan, K. A.; Yang, G.; Li, Z.; Fischer, E. S.; Treon, S. P.; Weinstock, D. M.; Gray, N. S. Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood 2019, 133 (9), 952-961. DOI: 10.1182/blood-2018-07-862953.
Brand, M.; Jiang, B.; Bauer, S.; Donovan, K. A.; Liang, Y.; Wang, E. S.; Nowak, R. P.; Yuan, J. C.; Zhang, T.; Kwiatkowski, N.; Muller, A. C.; Fischer, E. S.; Gray, N. S.; Winter, G. E. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol 2019, 26 (2), 300-306 e309. DOI: 10.1016/j.chembiol.2018.11.006.
Thinnes, C. C.; Lohans, C. T.; Abboud, M. I.; Yeh, T. L.; Tumber, A.; Nowak, R. P.; Attwood, M.; Cockman, M. E.; Oppermann, U.; Loenarz, C.; Schofield, C. J. Selective Inhibitors of a Human Prolyl Hydroxylase (OGFOD1) Involved in Ribosomal Decoding. Chemistry 2019, 25 (8), 2019-2024. DOI: 10.1002/chem.201804790.
de Wispelaere, M.; Du, G.; Donovan, K. A.; Zhang, T.; Eleuteri, N. A.; Yuan, J. C.; Kalabathula, J.; Nowak, R. P.; Fischer, E. S.; Gray, N. S.; Yang, P. L. Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nat Commun 2019, 10 (1), 3468. DOI: 10.1038/s41467-019-11429-w.
Morita, K.; He, S.; Nowak, R. P.; Wang, J.; Gray, N.; Fischer, E. S.; Look, A. T. Targeting T-ALL Cells with Potent Activators of the PP2A Protein Phosphatase Tumor Suppressor. American Society of Hematology Washington, DC: 2019.
Wright, N. D.; Collins, P.; Talon, R.; Nelson, E.; Koekemoer, L.; Ye, M.; Nowak, R.; Newman, J.; Ng, J. T.; Mitrovich, N. The low-cost, semi-automated shifter microscope stage transforms speed and robustness of manual protein crystal harvesting. bioRxiv 2019.
2018
Powell, C. E.; Gao, Y.; Tan, L.; Donovan, K. A.; Nowak, R. P.; Loehr, A.; Bahcall, M.; Fischer, E. S.; Janne, P. A.; George, R. E.; Gray, N. S. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). J Med Chem 2018, 61 (9), 4249-4255. DOI: 10.1021/acs.jmedchem.7b01655.
Zhou, W.; Whiteley, A. T.; de Oliveira Mann, C. C.; Morehouse, B. R.; Nowak, R. P.; Fischer, E. S.; Gray, N. S.; Mekalanos, J. J.; Kranzusch, P. J. Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell 2018, 174 (2), 300-311 e311. DOI: 10.1016/j.cell.2018.06.026.
Nowak, R. P.; DeAngelo, S. L.; Buckley, D.; He, Z.; Donovan, K. A.; An, J.; Safaee, N.; Jedrychowski, M. P.; Ponthier, C. M.; Ishoey, M.; Zhang, T.; Mancias, J. D.; Gray, N. S.; Bradner, J. E.; Fischer, E. S. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol 2018, 14 (7), 706-714. DOI: 10.1038/s41589-018-0055-y.
Donovan, K. A.; An, J.; Nowak, R. P.; Yuan, J. C.; Fink, E. C.; Berry, B. C.; Ebert, B. L.; Fischer, E. S. Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. Elife 2018, 7, e38430. DOI: 10.7554/eLife.38430.
Morrow, S.; Dobrovolsky, D.; Wang, E.; Nowak, R. P.; Donovan, K.; Faust, T.; Yang, G.; Li, Z.; Fischer, E.; Treon, S. P.; Weinstock, D. M.; Gray, N. S. Triple Degradation of BTK, IKZF1 and IKZF3 in B-Cell Malignancies. Blood 2018, 132, 263.
2017
Tarhonskaya, H.; Nowak, R. P.; Johansson, C.; Szykowska, A.; Tumber, A.; Hancock, R. L.; Lang, P.; Flashman, E.; Oppermann, U.; Schofield, C. J.; Kawamura, A. Studies on the Interaction of the Histone Demethylase KDM5B with Tricarboxylic Acid Cycle Intermediates. J Mol Biol 2017, 429 (19), 2895-2906. DOI: 10.1016/j.jmb.2017.08.007.
Tumber, A.; Nuzzi, A.; Hookway, E. S.; Hatch, S. B.; Velupillai, S.; Johansson, C.; Kawamura, A.; Savitsky, P.; Yapp, C.; Szykowska, A.; Wu, N.; Bountra, C.; Strain-Damerell, C.; Burgess-Brown, N. A.; Ruda, G. F.; Fedorov, O.; Munro, S.; England, K. S.; Nowak, R. P.; Schofield, C. J.; La Thangue, N. B.; Pawlyn, C.; Davies, F.; Morgan, G.; Athanasou, N.; Muller, S.; Oppermann, U.; Brennan, P. E. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol 2017, 24 (3), 371-380. DOI: 10.1016/j.chembiol.2017.02.006.
Pearce, N. M.; Krojer, T.; Bradley, A. R.; Collins, P.; Nowak, R. P.; Talon, R.; Marsden, B. D.; Kelm, S.; Shi, J.; Deane, C. M.; von Delft, F. A multi-crystal method for extracting obscured crystallographic states from conventionally uninterpretable electron density. Nat Commun 2017, 8 (1), 15123. DOI: 10.1038/ncomms15123.
2016
Johansson, C.; Velupillai, S.; Tumber, A.; Szykowska, A.; Hookway, E. S.; Nowak, R. P.; Strain-Damerell, C.; Gileadi, C.; Philpott, M.; Burgess-Brown, N.; Wu, N.; Kopec, J.; Nuzzi, A.; Steuber, H.; Egner, U.; Badock, V.; Munro, S.; LaThangue, N. B.; Westaway, S.; Brown, J.; Athanasou, N.; Prinjha, R.; Brennan, P. E.; Oppermann, U. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol 2016, 12 (7), 539-545. DOI: 10.1038/nchembio.2087.
Korczynska, M.; Le, D. D.; Younger, N.; Gregori-Puigjane, E.; Tumber, A.; Krojer, T.; Velupillai, S.; Gileadi, C.; Nowak, R. P.; Iwasa, E.; Pollock, S. B.; Ortiz Torres, I.; Oppermann, U.; Shoichet, B. K.; Fujimori, D. G. Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. J Med Chem 2016, 59 (4), 1580-1598. DOI: 10.1021/acs.jmedchem.5b01527.
Nowak, R. P.; Tumber, A.; Johansson, C.; Che, K. H.; Brennan, P.; Owen, D.; Oppermann, U. Advances and challenges in understanding histone demethylase biology. Curr Opin Chem Biol 2016, 33, 151-159. DOI: 10.1016/j.cbpa.2016.06.021.
Lobley, C. M.; Sandy, J.; Sanchez-Weatherby, J.; Mazzorana, M.; Krojer, T.; Nowak, R. P.; Sorensen, T. L. A generic protocol for protein crystal dehydration using the HC1b humidity controller. Acta Crystallographica Section D: Structural Biology 2016, 72 (5), 629-640.
Connor, A. J.; Nowak, R. P.; Lorenzon, E.; Thomas, M.; Herting, F.; Hoert, S.; Quaiser, T.; Shochat, E.; Pitt-Francis, J.; Cooper, J.; Maini, P. K.; Byrne, H. M. An integrated approach to quantitative modelling in angiogenesis research. J R Soc Interface 2015, 12 (110), 0546. DOI: 10.1098/rsif.2015.0546.
2015
Aik, W. S.; Chowdhury, R.; Clifton, I. J.; Hopkinson, R. J.; Leissing, T.; McDonough, M. A.; Nowak, R.; Schofield, C. J.; Walport, L. J. Introduction to structural studies on 2-oxoglutarate-dependent oxygenases and related enzymes. In 2-Oxoglutarate-dependent oxygenases, Royal Society of Chemistry Cambridge, UK, 2015; pp 59-94.
2014
Johansson, C.; Tumber, A.; Che, K.; Cain, P.; Nowak, R.; Gileadi, C.; Oppermann, U. The roles of Jumonji-type oxygenases in human disease. Epigenomics 2014, 6 (1), 89-120. DOI: 10.2217/epi.13.79.
Zou, C.; Yoon, H.; Park, P. M. C.; Patten, J. J.; Pellman, J.; Carreiro, J.; Tsai, J. M.; Li, Y. D.; Roy Burman, S. S.; Donovan, K. A.; Gasser, J.; Sperling, A. S.; Nowak, R. P.; Fischer, E. S.; Davey, R. A.; Ebert, B. L.; Slabicki, M. The human E3 ligase RNF185 is a regulator of the SARS-CoV-2 envelope protein. iScience 2023, 26 (5), 106601. DOI: 10.1016/j.isci.2023.106601.
Yue, H.; Nowak, R. P.; Overwijn, D.; Payne, N. C.; Fischinger, S.; Atyeo, C.; Lam, E. C.; St Denis, K.; Brais, L. K.; Konishi, Y.; Sklavenitis-Pistofidis, R.; Baden, L. R.; Nilles, E. J.; Karlson, E. W.; Yu, X. G.; Li, J. Z.; Woolley, A. E.; Ghobrial, I. M.; Meyerhardt, J. A.; Balazs, A. B.; Alter, G.; Mazitschek, R.; Fischer, E. S. Diagnostic TR-FRET assays for detection of antibodies in patient samples. Cell Rep Methods 2023, 3 (3), 100421. DOI: 10.1016/j.crmeth.2023.100421 From NLM Medline.
Nowak, R. P.; Che, J.; Ferrao, S.; Kong, N. R.; Liu, H.; Zerfas, B. L.; Jones, L. H. Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives. RSC Med Chem 2023, 14 (3), 501-506. DOI: 10.1039/d2md00347c From NLM PubMed-not-MEDLINE.
Perner, F.; Stein, E. M.; Wenge, D. V.; Singh, S.; Kim, J.; Apazidis, A.; Rahnamoun, H.; Anand, D.; Marinaccio, C.; Hatton, C.; Wen, Y.; Stone, R. M.; Schaller, D.; Mowla, S.; Xiao, W.; Gamlen, H. A.; Stonestrom, A. J.; Persaud, S.; Ener, E.; Cutler, J. A.; Doench, J. G.; McGeehan, G. M.; Volkamer, A.; Chodera, J. D.; Nowak, R. P.; Fischer, E. S.; Levine, R. L.; Armstrong, S. A.; Cai, S. F. MEN1 mutations mediate clinical resistance to menin inhibition. Nature 2023. DOI: 10.1038/s41586-023-05755-9.
Teng, M.; Jiang, J.; Wang, E. S.; Geng, Q.; Toenjes, S. T.; Donovan, K. A.; Mageed, N.; Yue, H.; Nowak, R. P.; Wang, J.; Manz, T. D.; Fischer, E. S.; Cantley, L. C.; Gray, N. S. Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader. Angew Chem Int Ed Engl 2023, e202302364. DOI: 10.1002/anie.202302364.
Hanzl, A.; Barone, E.; Bauer, S.; Yue, H.; Nowak, R. P.; Hahn, E.; Pankevich, E. V.; Koren, A.; Kubicek, S.; Fischer, E. S.; Winter, G. E. E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance. J Am Chem Soc 2023, 145 (2), 1176-1184. DOI: 10.1021/jacs.2c10784.
Li, J.; Wang, L.; Hahn, Q.; Nowak, R. P.; Viennet, T.; Orellana, E. A.; Roy Burman, S. S.; Yue, H.; Hunkeler, M.; Fontana, P.; Wu, H.; Arthanari, H.; Fischer, E. S.; Gregory, R. I. Structural basis of regulated m(7)G tRNA modification by METTL1-WDR4. Nature 2023, 613 (7943), 391-397. DOI: 10.1038/s41586-022-05566-4.
Boytz, R.; Slabicki, M.; Ramaswamy, S.; Patten, J. J.; Zou, C.; Meng, C.; Hurst, B. L.; Wang, J.; Nowak, R. P.; Yang, P. L.; Sattler, M.; Stone, R. M.; Griffin, J. D.; Gray, N. S.; Gummuluru, S.; Davey, R. A.; Weisberg, E. Anti-SARS-CoV-2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID-19 therapy. J Med Virol 2023, 95 (1), e28157. DOI: 10.1002/jmv.28157.
Tsang, T.; Huerta, F.; Liu, Y.; Che, J.; Metivier, R. J.; Ferrao, S.; Donovan, K. A.; Jones, L. H.; Zerfas, B. L.; Nowak, R. P. HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development. ACS Chem Biol 2023, 18 (4), 933-941. DOI: 10.1021/acschembio.3c00084.
Gao, Y.; Jiang, B.; Kim, H.; Berberich, M. J.; Che, J.; Donovan, K. A.; Hatcher, J. M.; Huerta, F.; Kwiatkowski, N. P.; Liu, Y.; Liuni, P. P.; Metivier, R. J.; Murali, V. K.; Nowak, R. P.; Zhang, T.; Fischer, E. S.; Gray, N. S.; Jones, L. H. Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions. J Med Chem 2023. DOI: 10.1021/acs.jmedchem.2c01864.
Cruite, J. T.; Nowak, R. P.; Donovan, K. A.; Ficarro, S. B.; Huang, H.; Liu, H.; Liu, Y.; Marto, J. A.; Metivier, R. J.; Fischer, E. S.; Jones, L. H. Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange. ACS Medicinal Chemistry Letters 2023. DOI: 10.1021/acsmedchemlett.3c00371.
Nowak, R. P.; Ragosta, L.; Huerta, F.; Liu, H.; Ficarro, S. B.; Cruite, J. T.; Metivier, R. J.; Donovan, K. A.; Marto, J. A.; Fischer, E. S.; Zerfas, B. L.; Jones, L. H. Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead. RSC Chemical Biology 2023, 10.1039/D3CB00103B. DOI: 10.1039/D3CB00103B.
2022
Verano, A. L.; You, I.; Donovan, K. A.; Mageed, N.; Yue, H.; Nowak, R. P.; Fischer, E. S.; Wang, E. S.; Gray, N. S. Redirecting the Neo-Substrate Specificity of Cereblon-Targeting PROTACs to Helios. ACS Chem Biol 2022, 17 (9), 2404-2410. DOI: 10.1021/acschembio.2c00439.
Aubrey, B. J.; Cutler, J. A.; Bourgeois, W.; Donovan, K. A.; Gu, S.; Hatton, C.; Perlee, S.; Perner, F.; Rahnamoun, H.; Theall, A. C. P.; Henrich, J. A.; Zhu, Q.; Nowak, R. P.; Kim, Y. J.; Parvin, S.; Cremer, A.; Olsen, S. N.; Eleuteri, N. A.; Pikman, Y.; McGeehan, G. M.; Stegmaier, K.; Letai, A.; Fischer, E. S.; Liu, X. S.; Armstrong, S. A. IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia. Nat Cancer 2022, 3 (5), 595-613. DOI: 10.1038/s43018-022-00366-1.
Cruite, J. T.; Dann, G. P.; Che, J.; Donovan, K. A.; Ferrao, S.; Ficarro, S. B.; Fischer, E. S.; Gray, N. S.; Huerta, F.; Kong, N. R.; Liu, H.; Marto, J. A.; Metivier, R. J.; Nowak, R. P.; Zerfas, B. L.; Jones, L. H. Cereblon covalent modulation through structure-based design of histidine targeting chemical probes. RSC Chem Biol 2022, 3 (9), 1105-1110. DOI: 10.1039/d2cb00078d.
Du, G.; Jiang, J.; Henning, N. J.; Safaee, N.; Koide, E.; Nowak, R. P.; Donovan, K. A.; Yoon, H.; You, I.; Yue, H.; Eleuteri, N. A.; He, Z.; Li, Z.; Huang, H. T.; Che, J.; Nabet, B.; Zhang, T.; Fischer, E. S.; Gray, N. S. Exploring the target scope of KEAP1 E3 ligase-based PROTACs. Cell Chem Biol 2022. DOI: 10.1016/j.chembiol.2022.08.003.
Dann, G. P.; Liu, H.; Nowak, R. P.; Jones, L. H. Cereblon target validation using a covalent inhibitor of neosubstrate recruitment. In Methods in Enzymology, Academic Press, 2022.
Zerfas, B. L.; Huerta, F.; Liu, H.; Du, G.; Gray, N. S.; Jones, L. H.; Nowak, R. P. Advancing targeted protein degrader discovery by measuring cereblon engagement in cells. In Methods in Enzymology, Academic Press, 2022.
Meyerhardt, J. A.; Yue, H.; Nowak, R. P.; Brais, L.; Ma, C.; Johnson, S.; Harrod, J.; Burman, S. S. R.; Hendrickson, L. M.; Fischinger, S.; Alter, G.; Hahn, W.; Johnson, B. E.; Fischer, E. S. Serological testing for SARS-CoV-2 antibodies of employees shows low transmission working in a cancer center. PLoS One 2022, 17 (4), e0266791. DOI: 10.1371/journal.pone.0266791.
Silva, M. C.; Nandi, G.; Donovan, K. A.; Cai, Q.; Berry, B. C.; Nowak, R. P.; Fischer, E. S.; Gray, N. S.; Ferguson, F. M.; Haggarty, S. J. Discovery and Optimization of Tau Targeted Protein Degraders Enabled by Patient Induced Pluripotent Stem Cells-Derived Neuronal Models of Tauopathy. Front Cell Neurosci 2022, 16, 801179. DOI: 10.3389/fncel.2022.801179.
2021
Dubey, A.; Stoyanov, N.; Viennet, T.; Chhabra, S.; Elter, S.; Borggrafe, J.; Viegas, A.; Nowak, R. P.; Burdzhiev, N.; Petrov, O.; Fischer, E. S.; Etzkorn, M.; Gelev, V.; Arthanari, H. Local Deuteration Enables NMR Observation of Methyl Groups in Proteins from Eukaryotic and Cell-Free Expression Systems. Angew Chem Int Ed Engl 2021, 60 (25), 13783-13787. DOI: 10.1002/anie.202016070.
Wang, E. S.; Verano, A. L.; Nowak, R. P.; Yuan, J. C.; Donovan, K. A.; Eleuteri, N. A.; Yue, H.; Ngo, K. H.; Lizotte, P. H.; Gokhale, P. C.; Gray, N. S.; Fischer, E. S. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol 2021, 17 (6), 711-717. DOI: 10.1038/s41589-021-00802-w.
Xiong, Y.; Donovan, K. A.; Eleuteri, N. A.; Kirmani, N.; Yue, H.; Razov, A.; Krupnick, N. M.; Nowak, R. P.; Fischer, E. S. Chemo-proteomics exploration of HDAC degradability by small molecule degraders. Cell Chem Biol 2021. DOI: 10.1016/j.chembiol.2021.07.002.
Fischer, P. D.; Papadopoulos, E.; Dempersmier, J. M.; Wang, Z. F.; Nowak, R. P.; Donovan, K. A.; Kalabathula, J.; Gorgulla, C.; Junghanns, P. P. M.; Kabha, E.; Dimitrakakis, N.; Petrov, O. I.; Mitsiades, C.; Ducho, C.; Gelev, V.; Fischer, E. S.; Wagner, G.; Arthanari, H. A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders. Eur J Med Chem 2021, 219, 113435. DOI: 10.1016/j.ejmech.2021.113435.
Wright, N. D.; Collins, P.; Koekemoer, L.; Krojer, T.; Talon, R.; Nelson, E.; Ye, M.; Nowak, R.; Newman, J.; Ng, J. T.; Mitrovich, N.; Wiggers, H.; von Delft, F. The low-cost Shifter microscope stage transforms the speed and robustness of protein crystal harvesting. Acta Crystallogr D Struct Biol 2021, 77 (Pt 1), 62-74. DOI: 10.1107/S2059798320014114.
Teng, M.; Lu, W.; Donovan, K. A.; Sun, J.; Krupnick, N. M.; Nowak, R. P.; Li, Y. D.; Sperling, A. S.; Zhang, T.; Ebert, B. L.; Fischer, E. S.; Gray, N. S. Development of PDE6D and CK1alpha Degraders through Chemical Derivatization of FPFT-2216. J Med Chem 2021. DOI: 10.1021/acs.jmedchem.1c01832.
Wu, W.; Nelson, G.; Koch, R.; Donovan, K. A.; Nowak, R. P.; Heavican-Foral, T. B.; Nirmal, A. J.; Liu, H.; Yang, L.; Duffy, J.; Powers, F.; Stevenson, K. E.; Jones, M.; Ng, S. Y.; Wu, G.; Jain, S.; Xu, R.; Amaka, S.; Trevisani, C.; Donaldson, N.; Hagner, P. R.; de Leval, L.; Gaulard, P.; Iqbal, J.; Thakurta, A.; Fischer, E. S.; Adelman, K.; Weinstock, D. M. Overcoming IMiD Resistance in T-cell Lymphomas Through Potent Degradation of ZFP91 and IKZF1. Blood 2021. DOI: 10.1182/blood.2021014701.
Konishi, Y.; Sklavenitis-Pistofidis, R.; Yue, H.; Ferrari, F.; Redd, R. A.; Lightbody, E. D.; Russo, M.; Perry, J.; Horowitz, E.; Justis, A. V.; Shayegh, N. A.; Savell, A.; Prescott, J.; Varmeh, S.; Nowak, R. P.; Hamilton, M.; Auclair, D.; Marinac, C. R.; Trippa, L.; Fischer, E. S.; Ghobrial, I. M. Attenuated response to SARS-CoV-2 vaccine in patients with asymptomatic precursor stages of multiple myeloma and Waldenstrom macroglobulinemia. Cancer Cell 2021. DOI: 10.1016/j.ccell.2021.12.003.
Nowak, R. P.; Xiong, Y.; Kirmani, N.; Kalabathula, J.; Donovan, K. A.; Eleuteri, N. A.; Yuan, J. C.; Fischer, E. S. Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. J Med Chem 2021, 64 (15), 11637-11650. DOI: 10.1021/acs.jmedchem.1c00958.
Nowak, R. P.; Jones, L. H. Target Validation Using PROTACs: Applying the Four Pillars Framework. SLAS DISCOVERY: Advancing the Science of Drug Discovery 2021, 26 (4), 474-483.
Nowak, R. P.; Yue, H.; Park, E. Y.; Fischer, E. S. Methods for Quantitative Assessment of Protein Degradation. Methods Mol Biol 2021, 2365, 247-263. DOI: 10.1007/978-1-0716-1665-9_13.
2020
Powell, C. E.; Du, G.; Che, J.; He, Z.; Donovan, K. A.; Yue, H.; Wang, E. S.; Nowak, R. P.; Zhang, T.; Fischer, E. S.; Gray, N. S. Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. ACS Chem Biol 2020, 15 (10), 2722-2730. DOI: 10.1021/acschembio.0c00520.
Li, Z.; Pinch, B. J.; Olson, C. M.; Donovan, K. A.; Nowak, R. P.; Mills, C. E.; Scott, D. A.; Doctor, Z. M.; Eleuteri, N. A.; Chung, M.; Sorger, P. K.; Fischer, E. S.; Gray, N. S. Development and Characterization of a Wee1 Kinase Degrader. Cell Chem Biol 2020, 27 (1), 57-65 e59. DOI: 10.1016/j.chembiol.2019.10.013.
Zeng, M.; Xiong, Y.; Safaee, N.; Nowak, R. P.; Donovan, K. A.; Yuan, C. J.; Nabet, B.; Gero, T. W.; Feru, F.; Li, L.; Gondi, S.; Ombelets, L. J.; Quan, C.; Janne, P. A.; Kostic, M.; Scott, D. A.; Westover, K. D.; Fischer, E. S.; Gray, N. S. Exploring Targeted Degradation Strategy for Oncogenic KRAS(G12C). Cell Chem Biol 2020, 27 (1), 19-31 e16. DOI: 10.1016/j.chembiol.2019.12.006.
Faust, T. B.; Yoon, H.; Nowak, R. P.; Donovan, K. A.; Li, Z.; Cai, Q.; Eleuteri, N. A.; Zhang, T.; Gray, N. S.; Fischer, E. S. Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nat Chem Biol 2020, 16 (1), 7-14. DOI: 10.1038/s41589-019-0378-3.
Slabicki, M.; Yoon, H.; Koeppel, J.; Nitsch, L.; Roy Burman, S. S.; Di Genua, C.; Donovan, K. A.; Sperling, A. S.; Hunkeler, M.; Tsai, J. M.; Sharma, R.; Guirguis, A.; Zou, C.; Chudasama, P.; Gasser, J. A.; Miller, P. G.; Scholl, C.; Frohling, S.; Nowak, R. P.; Fischer, E. S.; Ebert, B. L. Small-molecule-induced polymerization triggers degradation of BCL6. Nature 2020, 588 (7836), 164-168. DOI: 10.1038/s41586-020-2925-1.
Jang, J.; To, C.; De Clercq, D. J. H.; Park, E.; Ponthier, C. M.; Shin, B. H.; Mushajiang, M.; Nowak, R. P.; Fischer, E. S.; Eck, M. J.; Janne, P. A.; Gray, N. S. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl 2020, 59 (34), 14481-14489. DOI: 10.1002/anie.202003500.
Morita, K.; He, S.; Nowak, R. P.; Wang, J.; Zimmerman, M. W.; Fu, C.; Durbin, A. D.; Martel, M. W.; Prutsch, N.; Gray, N. S.; Fischer, E. S.; Look, A. T. Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell 2020, 181 (3), 702-715 e720. DOI: 10.1016/j.cell.2020.03.051.
Gasic, I.; Groendyke, B. J.; Nowak, R. P.; Yuan, J. C.; Kalabathula, J.; Fischer, E. S.; Gray, N. S.; Mitchison, T. J. Tubulin Resists Degradation by Cereblon-Recruiting PROTACs. Cells 2020, 9 (5), 1083. DOI: 10.3390/cells9051083.
Yue, H.; Nowak, R. P.; Overwijn, D.; Payne, N. C.; Fischinger, S.; Atyeo, C.; Baden, L. R.; Nilles, E. J.; Karlson, E. W.; Xu, G. Y. Rapid'mix and read'assay for scalable detection of SARS-CoV-2 antibodies in patient plasma. medRxiv 2020.
Wu, T.; Yoon, H.; Xiong, Y.; Dixon-Clarke, S. E.; Nowak, R. P.; Fischer, E. S. Targeted protein degradation as a powerful research tool in basic biology and drug target discovery. Nature Structural & Molecular Biology 2020, 27 (7), 605-614.
2019
Dobrovolsky, D.; Wang, E. S.; Morrow, S.; Leahy, C.; Faust, T.; Nowak, R. P.; Donovan, K. A.; Yang, G.; Li, Z.; Fischer, E. S.; Treon, S. P.; Weinstock, D. M.; Gray, N. S. Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood 2019, 133 (9), 952-961. DOI: 10.1182/blood-2018-07-862953.
Brand, M.; Jiang, B.; Bauer, S.; Donovan, K. A.; Liang, Y.; Wang, E. S.; Nowak, R. P.; Yuan, J. C.; Zhang, T.; Kwiatkowski, N.; Muller, A. C.; Fischer, E. S.; Gray, N. S.; Winter, G. E. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol 2019, 26 (2), 300-306 e309. DOI: 10.1016/j.chembiol.2018.11.006.
Thinnes, C. C.; Lohans, C. T.; Abboud, M. I.; Yeh, T. L.; Tumber, A.; Nowak, R. P.; Attwood, M.; Cockman, M. E.; Oppermann, U.; Loenarz, C.; Schofield, C. J. Selective Inhibitors of a Human Prolyl Hydroxylase (OGFOD1) Involved in Ribosomal Decoding. Chemistry 2019, 25 (8), 2019-2024. DOI: 10.1002/chem.201804790.
de Wispelaere, M.; Du, G.; Donovan, K. A.; Zhang, T.; Eleuteri, N. A.; Yuan, J. C.; Kalabathula, J.; Nowak, R. P.; Fischer, E. S.; Gray, N. S.; Yang, P. L. Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nat Commun 2019, 10 (1), 3468. DOI: 10.1038/s41467-019-11429-w.
Morita, K.; He, S.; Nowak, R. P.; Wang, J.; Gray, N.; Fischer, E. S.; Look, A. T. Targeting T-ALL Cells with Potent Activators of the PP2A Protein Phosphatase Tumor Suppressor. American Society of Hematology Washington, DC: 2019.
Wright, N. D.; Collins, P.; Talon, R.; Nelson, E.; Koekemoer, L.; Ye, M.; Nowak, R.; Newman, J.; Ng, J. T.; Mitrovich, N. The low-cost, semi-automated shifter microscope stage transforms speed and robustness of manual protein crystal harvesting. bioRxiv 2019.
2018
Powell, C. E.; Gao, Y.; Tan, L.; Donovan, K. A.; Nowak, R. P.; Loehr, A.; Bahcall, M.; Fischer, E. S.; Janne, P. A.; George, R. E.; Gray, N. S. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). J Med Chem 2018, 61 (9), 4249-4255. DOI: 10.1021/acs.jmedchem.7b01655.
Zhou, W.; Whiteley, A. T.; de Oliveira Mann, C. C.; Morehouse, B. R.; Nowak, R. P.; Fischer, E. S.; Gray, N. S.; Mekalanos, J. J.; Kranzusch, P. J. Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell 2018, 174 (2), 300-311 e311. DOI: 10.1016/j.cell.2018.06.026.
Nowak, R. P.; DeAngelo, S. L.; Buckley, D.; He, Z.; Donovan, K. A.; An, J.; Safaee, N.; Jedrychowski, M. P.; Ponthier, C. M.; Ishoey, M.; Zhang, T.; Mancias, J. D.; Gray, N. S.; Bradner, J. E.; Fischer, E. S. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol 2018, 14 (7), 706-714. DOI: 10.1038/s41589-018-0055-y.
Donovan, K. A.; An, J.; Nowak, R. P.; Yuan, J. C.; Fink, E. C.; Berry, B. C.; Ebert, B. L.; Fischer, E. S. Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. Elife 2018, 7, e38430. DOI: 10.7554/eLife.38430.
Morrow, S.; Dobrovolsky, D.; Wang, E.; Nowak, R. P.; Donovan, K.; Faust, T.; Yang, G.; Li, Z.; Fischer, E.; Treon, S. P.; Weinstock, D. M.; Gray, N. S. Triple Degradation of BTK, IKZF1 and IKZF3 in B-Cell Malignancies. Blood 2018, 132, 263.
2017
Tarhonskaya, H.; Nowak, R. P.; Johansson, C.; Szykowska, A.; Tumber, A.; Hancock, R. L.; Lang, P.; Flashman, E.; Oppermann, U.; Schofield, C. J.; Kawamura, A. Studies on the Interaction of the Histone Demethylase KDM5B with Tricarboxylic Acid Cycle Intermediates. J Mol Biol 2017, 429 (19), 2895-2906. DOI: 10.1016/j.jmb.2017.08.007.
Tumber, A.; Nuzzi, A.; Hookway, E. S.; Hatch, S. B.; Velupillai, S.; Johansson, C.; Kawamura, A.; Savitsky, P.; Yapp, C.; Szykowska, A.; Wu, N.; Bountra, C.; Strain-Damerell, C.; Burgess-Brown, N. A.; Ruda, G. F.; Fedorov, O.; Munro, S.; England, K. S.; Nowak, R. P.; Schofield, C. J.; La Thangue, N. B.; Pawlyn, C.; Davies, F.; Morgan, G.; Athanasou, N.; Muller, S.; Oppermann, U.; Brennan, P. E. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol 2017, 24 (3), 371-380. DOI: 10.1016/j.chembiol.2017.02.006.
Pearce, N. M.; Krojer, T.; Bradley, A. R.; Collins, P.; Nowak, R. P.; Talon, R.; Marsden, B. D.; Kelm, S.; Shi, J.; Deane, C. M.; von Delft, F. A multi-crystal method for extracting obscured crystallographic states from conventionally uninterpretable electron density. Nat Commun 2017, 8 (1), 15123. DOI: 10.1038/ncomms15123.
2016
Johansson, C.; Velupillai, S.; Tumber, A.; Szykowska, A.; Hookway, E. S.; Nowak, R. P.; Strain-Damerell, C.; Gileadi, C.; Philpott, M.; Burgess-Brown, N.; Wu, N.; Kopec, J.; Nuzzi, A.; Steuber, H.; Egner, U.; Badock, V.; Munro, S.; LaThangue, N. B.; Westaway, S.; Brown, J.; Athanasou, N.; Prinjha, R.; Brennan, P. E.; Oppermann, U. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol 2016, 12 (7), 539-545. DOI: 10.1038/nchembio.2087.
Korczynska, M.; Le, D. D.; Younger, N.; Gregori-Puigjane, E.; Tumber, A.; Krojer, T.; Velupillai, S.; Gileadi, C.; Nowak, R. P.; Iwasa, E.; Pollock, S. B.; Ortiz Torres, I.; Oppermann, U.; Shoichet, B. K.; Fujimori, D. G. Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. J Med Chem 2016, 59 (4), 1580-1598. DOI: 10.1021/acs.jmedchem.5b01527.
Nowak, R. P.; Tumber, A.; Johansson, C.; Che, K. H.; Brennan, P.; Owen, D.; Oppermann, U. Advances and challenges in understanding histone demethylase biology. Curr Opin Chem Biol 2016, 33, 151-159. DOI: 10.1016/j.cbpa.2016.06.021.
Lobley, C. M.; Sandy, J.; Sanchez-Weatherby, J.; Mazzorana, M.; Krojer, T.; Nowak, R. P.; Sorensen, T. L. A generic protocol for protein crystal dehydration using the HC1b humidity controller. Acta Crystallographica Section D: Structural Biology 2016, 72 (5), 629-640.
Connor, A. J.; Nowak, R. P.; Lorenzon, E.; Thomas, M.; Herting, F.; Hoert, S.; Quaiser, T.; Shochat, E.; Pitt-Francis, J.; Cooper, J.; Maini, P. K.; Byrne, H. M. An integrated approach to quantitative modelling in angiogenesis research. J R Soc Interface 2015, 12 (110), 0546. DOI: 10.1098/rsif.2015.0546.
2015
Aik, W. S.; Chowdhury, R.; Clifton, I. J.; Hopkinson, R. J.; Leissing, T.; McDonough, M. A.; Nowak, R.; Schofield, C. J.; Walport, L. J. Introduction to structural studies on 2-oxoglutarate-dependent oxygenases and related enzymes. In 2-Oxoglutarate-dependent oxygenases, Royal Society of Chemistry Cambridge, UK, 2015; pp 59-94.
2014
Johansson, C.; Tumber, A.; Che, K.; Cain, P.; Nowak, R.; Gileadi, C.; Oppermann, U. The roles of Jumonji-type oxygenases in human disease. Epigenomics 2014, 6 (1), 89-120. DOI: 10.2217/epi.13.79.