Publications

  • Mohamed, W. I., Park, S. L., Rabl, J., Leitner, A., Boehringer, D., Peter, M. (2021). The human GID complex engages two independent modules for substrate recruitment. EMBO reports, e52981. Advance online publication.

  • Cichońska, A., Ravikumar, B., Allaway, R. J., Wan, F., Park, S., Isayev, O., Li, S., Mason, M., Lamb, A., Tanoli, Z., Jeon, M., Kim, S., Popova, M., Capuzzi, S., Zeng, J., Dang, K., Koytiger, G., Kang, J., Wells, C. I., Willson, T. M., … Aittokallio, T. (2021). Crowdsourced mapping of unexplored target space of kinase inhibitors. Nature communications12(1), 3307.

  • Krojer, T., Fraser, J. S., & von Delft, F. (2020). Discovery of allosteric binding sites by crystallographic fragment screening. Current opinion in structural biology, 65, 209–216.

  • Baker, L., Aimon, A., Murray, J., Surgenor, A., Matassova, N., Roughley, S., ... Hubbard, R. (2020). Rapid optimisation of fragments and hits to lead compounds from screening of crude reaction mixtures. Communications Chemistry, 3(1).

  • Kidd, S., Fowler, E., Reinhardt, T., Compton, T., Mateu, N., Newman, H., ... Spring, D. (2020). Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion. Chemical Science, 11(39), 10792-10801.

  • Sundström, Y., Shang, M. M., Panda, S. K., Grönwall, C., Wermeling, F., Gunnarsson, I., ... Berg, L. (2020). Identifying novel B-cell targets for chronic inflammatory autoimmune disease by screening of chemical probes in a patient-derived cell assay. Transl Res. S1931-5244(20)30225-5.

  • Cottone, L., Cribbs, A., Khandelwal, G., Wells, G., Ligammari, L., Philpott, M., ... Flanagan, A. (2020). Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death. Cancer Research, 80(20), 4540-4551.

  • Williams, L., McCann, F., Cabrita, M., Layton, T., Cribbs, A., Knezevic, B., ... Nanchahal, J. (2020). Identifying collagen VI as a target of fibrotic diseases regulated by CREBBP/EP300. Proceedings Of The National Academy Of Sciences, 117(34), 20753-20763.

  • Quevedo, C. E., Bataille, C., Byrne, S., Durbin, M., Elkins, J., Guillermo, A., ... Russell, A. J. (2020). Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family. Bioorganic & medicinal chemistry, 28(22), 115724.

  • Iyer, V., Jiang, L., Shen, Y., Boddul, S., Panda, S., Kasza, Z., ... Wermeling, F. (2020). Designing custom CRISPR libraries for hypothesis-driven drug target discovery. Computational And Structural Biotechnology Journal, 18, 2237-2246.

  • Smil, D., Wong, J. F., Williams, E. P., Adamson, R. J., Howarth, A., McLeod, D. A., ... Isaac, M. B. (2020). Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. Journal of medicinal chemistry, 63(17), 10061–10085.

  • Buljan, M., Ciuffa, R., van Drogen, A., Vichalkovski, A., Mehnert, M., Rosenberger, G., . . . Gstaiger, M. (2020). Kinase Interaction Network Expands Functional and Disease Roles of Human Kinases. Mol Cell, 79(3), 504-520.e509

  • Marques, J. G., Gryder, B. E., Pavlovic, B., Chung, Y., Ngo, Q. A., Frommelt, F., . . . Schäfer, B. W. (2020). NuRD subunit CHD4 regulates super-enhancer accessibility in rhabdomyosarcoma and represents a general tumor dependency. Elife, 9.

  • Marques, J. G., Gryder, B. E., Pavlovic, B., Chung, Y., Ngo, Q. A., Frommelt, F., Gstaiger, M., Song, Y., Benischke, K., Laubscher, D., Wachtel, M., Khan, J., & Schäfer, B. W. (2020). NuRD subunit CHD4 regulates super-enhancer accessibility in rhabdomyosarcoma and represents a general tumor dependency. eLife9, e54993.

  • Kock, A., Bergqvist, F., Steinmetz, J., Elfman, L. H. M., Korotkova, M., Johnsen, J. I., . . . Larsson, K. (2020). Establishment of an in vitro 3D model for neuroblastoma enables preclinical investigation of combined tumor-stroma drug targeting. Faseb j, 34(8), 11101-11114.

  • Mehnert, M., Ciuffa, R., Frommelt, F., Uliana, F., van Drogen, A., Ruminski, K., . . . Aebersold, R. (2020). Multi-layered proteomic analyses decode compositional and functional effects of cancer mutations on kinase complexes. Nat Commun, 11(1), 3563.

  • Henderson, S. H., Sorrell, F., Bennett, J., Hanley, M. T., Robinson, S., Hopkins Navratilova, I., ... Ward, S. E. (2020). Mining Public Domain Data to Develop Selective DYRK1A Inhibitors. ACS medicinal chemistry letters, 11(8), 1620–1626.

  • Chen, Z., Zhang, J., Heilig, R., Sorrell, F., D’Angiolella, V., Fischer, R., ... Bullock, A. N. (2020). Sequence and structural variations determining the recruitment of WNK kinases to the KLHL3 E3 ligase. Cold Spring Harbor Laboratory

  • Chen, Z., Wasney, G. A., Picaud, S., Filippakopoulos, P., Vedadi, M., D'Angiolella, V., & Bullock, A. N. (2020). Identification of a PGXPP degron motif in dishevelled and structural basis for its binding to the E3 ligase KLHL12. Open biology, 10(6), 200041.

  • Wells, C. I., Vasta, J. D., Corona, C. R., Wilkinson, J., Zimprich, C. A., Ingold, M. R., ... Robers, M. B. (2020). Quantifying CDK inhibitor selectivity in live cells. Nature communications, 11(1), 2743.

  • Shen, Y., Li, F., Szewczyk, M. M., Halabelian, L., Park, K. S., Chau, I., Dong, A., ... Jin, J. (2020). Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. Journal of medicinal chemistry, 63(10), 5477–5487.

  • Asquith, C., Tizzard, G. J., Bennett, J. M., Wells, C. I., Elkins, J. M., Willson, T. M., ... Laitinen, T. (2020). Targeting the Water Network in Cyclin G-Associated Kinase (GAK) with 4-Anilino-quin(az)oline Inhibitors. ChemMedChem, 15(13), 1200–1215.

  • Ensan, D., Smil, D., Zepeda-Velázquez, C. A., Panagopoulos, D., Wong, J. F., Williams, E. P., ... Al-Awar, R. (2020). Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma. Journal of medicinal chemistry, 63(9), 4978–4996.

  • Bergqvist, F., Sundström, Y., Shang, M. M., Gunnarsson, I., Lundberg, I. E., Sundström, M., . . . Berg, L. (2020). Anti-Inflammatory Properties of Chemical Probes in Human Whole Blood: Focus on Prostaglandin E(2) Production. Front Pharmacol, 11, 613

  • Rödström, K., Kiper, A. K., Zhang, W., Rinné, S., Pike, A., Goldstein, M., ... Carpenter, E. P. (2020). A lower X-gate in TASK channels traps inhibitors within the vestibule. Nature, 582(7812), 443–447.

  • Caplan, T., Lorente-Macías, Á., Stogios, P., Evdokimova, E., Hyde, S., Wellington, M., ... Cowen L. (2020). Overcoming Fungal Echinocandin Resistance through Inhibition of the Non-essential Stress Kinase Yck2. Cell Chemical Biology.

  • Fortin, J., Tian, R., Zarrabi, I., Hill, G., Williams, E., Sanchez-Duffhues, G., ... Mak, T. W. (2020). Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas. Cancer cell, 37(3), 308–323.e12.

  • Emmerich, A. C., Wellstein, J., Ossipova, E., Baumann, I., Lengqvist, J., Kultima, K., . . . Saul, M. J. (2020). Proteomics-Based Characterization of miR-574-5p Decoy to CUGBP1 Suggests Specificity for mPGES-1 Regulation in Human Lung Cancer Cells. Front Pharmacol, 11, 196

  • Stefaniak, J., & Huber, K. (2020). Importance of Quantifying Drug-Target Engagement in Cells. ACS medicinal chemistry letters, 11(4), 403–406.

  • Heusel, M., Frank, M., Köhler, M., Amon, S., Frommelt, F., Rosenberger, G., ... Aebersold, R. (2020). A Global Screen for Assembly State Changes of the Mitotic Proteome by SEC-SWATH-MS. Cell Syst, 10(2), 133-155.e136.

  • Ferla, M. P., Pagnamenta, A. T., Damerell, D., Taylor, J. C., & Marsden, B. D. (2020). MichelaNglo: sculpting protein views on web pages without coding. Bioinformatics (Oxford, England), 36(10), 3268–3270.

  • Panda, S., Wigerblad, G., Jiang, L., Jiménez-Andrade, Y., Iyer, V., Shen, Y., ... Wermeling, F. (2020). IL-4 controls activated neutrophil FcγR2b expression and migration into inflamed joints. Proceedings Of The National Academy Of Sciences, 117(6), 3103-3113.

  • Wang, Q., Corey, R. A., Hedger, G., Aryal, P., Grieben, M., Nasrallah, C., … Sansom, M. S. (2019). Lipid Interactions of a Ciliary Membrane TRP Channel: Simulation and Structural Studies of Polycystin-2. Structure, 28(2), 169-184.e5.

  • Newman, J. A., Aitkenhead, H., Gavard, A. E., Rota, I. A., Handel, A. E., Hollander, G. A., & Gileadi, O. (2019). The crystal structure of human forkhead box N1 in complex with DNA reveals the structural basis for forkhead box family specificity. Journal of Biological Chemistry, 295(10), 2948–2958.

  • Larsson, K., Steinmetz, J., Bergqvist, F., Arefin, S., Spahiu, L., Wannberg, J., … Jakobsson, P. J. (2019). Biological characterization of new inhibitors of microsomal PGE synthase‐1 in preclinical models of inflammation and vascular tone. British Journal of Pharmacology, 176(24), 4625–4638.

  • Allali-Hassani, A., Szewczyk, M. M., Ivanochko, D., Organ, S. L., Bok, J., Ho, J., … Vedadi, M. (2019). Discovery of a chemical probe for PRDM9. Nature communications, 10(1), 5759.

  • Ni, X., Heidenreich, D., Christott, T., Bennett, J., Moustakim, M., Brennan, P., ... Chaikuad A. (2019). Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1. ACS Medicinal Chemistry Letters, 10(12), 1661-1666.

  • Huang, Y., Mouttet, B., Warnatz, H., Risch, T., Rietmann, F., Frommelt, F., ... Bourquin, J. (2019). The Leukemogenic TCF3-HLF Complex Rewires Enhancers Driving Cellular Identity and Self-Renewal Conferring EP300 Vulnerability. Cancer Cell, 36(6), 630-644.e9.

  • Chaikuad, A., Thangaratnarajah, C., von Delft, F., & Bullock, A. N. (2019). Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension. Scientific reports, 9(1), 18351.

  • Li, A., Li, F., Eram, M., Bolotokova, A., dela Seña, C., & Vedadi, M. (2019). Chemical probes for protein arginine methyltransferases. Methods.

  • Sánchez-Duffhues, G., Williams, E., Benderitter, P., Orlova, V., van Wijhe, M., Garcia de Vinuesa, A., … Ten Dijke, P. (2019). Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva-Derived Endothelial Cells. JBMR plus, 3(11), e10230.

  • Ozyerli-Goknar, E., Sur-Erdem, I., Seker, F., Cingöz, A., Kayabolen, A., Kahya-Yesil, Z., … Bagci-Onder, T. (2019). The fungal metabolite chaetocin is a sensitizer for pro-apoptotic therapies in glioblastoma. Cell death & disease, 10(12), 894.

  • Shukla, V., Halabelian, L., Balagere, S., Samaniego-Castruita, D., Feldman, D., Arrowsmith, C., ... Aravind, L. (2020). HMCES Functions in the Alternative End-Joining Pathway of the DNA DSB Repair during Class Switch Recombination in B Cells. Molecular Cell, 77(2), 384-394.e4.

  • Profeta, G. S., Dos Reis, C. V., Santiago, A., Godoi, P., Fala, A. M., Wells, C. I., … Couñago, R. M. (2019). Binding and structural analyses of potent inhibitors of the human Ca2+/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors. Scientific reports, 9(1), 16452.

  • Kirkby, N., Raouf, J., Ahmetaj-Shala, B., Liu, B., Mazi, S., Edin, M., ... Mitchell, J. (2019). Mechanistic definition of the cardiovascular mPGES-1/COX-2/ADMA axis. Cardiovascular Research.

  • Bergqvist, F., Morgenstern, R., & Jakobsson, P. J. (2020). A review on mPGES-1 inhibitors: From preclinical studies to clinical applications. Prostaglandins & Other Lipid Mediators, 147, 106383.

  • Wei, Y., Resetca, D., Li, Z., Johansson-Åkhe, I., Ahlner, A., Helander, S., ... Sunnerhagen, M. (2019). Multiple direct interactions of TBP with the MYC oncoprotein. Nature Structural & Molecular Biology, 26(11), 1035-1043.

  • Asquith, C., Laitinen, T., Bennett, J., Wells, C., Elkins, J., Zuercher, W., ... Poso, A. (2019). Design and Analysis of the 4‐Anilinoquin(az)oline Kinase Inhibition Profiles of GAK/SLK/STK10 Using Quantitative Structure‐Activity Relationships. Chemmedchem, 15(1), 26-49.

  • Schapira, M., Calabrese, M., Bullock, A., & Crews, C. (2019). Targeted protein degradation: expanding the toolbox. Nature Reviews Drug Discovery, 18(12), 949-963.

  • Cai, X. C., Zhang, T., Kim, E. J., Jiang, M., Wang, K., Wang, J., … Luo, M. (2019). A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion. eLife, 8, e47110.

  • Liu, K., & Min, J. (2019). Structural Basis for the Recognition of Non-methylated DNA by the CXXC Domain. Journal Of Molecular Biology.

  • Carabajal, M., Asquith, C., Laitinen, T., Tizzard, G., Yim, L., Rial, A., ... García Véscovi, E. (2019). Quinazoline-Based Antivirulence Compounds Selectively Target Salmonella PhoP/PhoQ Signal Transduction System. Antimicrobial Agents And Chemotherapy, 64(1).

  • Salah, E., Chatterjee, D., Beltrami, A., Tumber, A., Preuss, F., Canning, P., … Mathea, S. (2019). Lessons from LIMK1 enzymology and their impact on inhibitor design. The Biochemical journal, 476(21), 3197–3209.

  • Yu, X., Plotnikova, O., Bonin, P. D., Subashi, T. A., McLellan, T. J., Dumlao, D., … Han, S. (2019). Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation. eLife, 8, e48120.

  • Barsyte-Lovejoy D. (2019). SETD7 at the heart of chromatin factor interplay. Stem cell investigation, 6, 20.

  • Fagan, V., Johansson, C., Gileadi, C., Monteiro, O., Dunford, J., Nibhani, R., ... Oppermann, U. (2019). A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function. Journal Of Medicinal Chemistry, 62(20), 9008-9025.

  • Wong, J. F., Brown, E. J., Williams, E., & Bullock, A. N. (2019). Fostering open collaboration in drug development for paediatric brain tumours. Biochemical Society transactions, 47(5), 1471–1479.

  • Righetto, G. L., Sriranganadane, D., Halabelian, L., Chiodi, C. G., Elkins, J. M., Massirer, K. B., … Couñago, R. M. (2019). The C-Terminal Domains SnRK2 Box and ABA Box Have a Role in Sugarcane SnRK2s Auto-Activation and Activity. Frontiers in plant science, 10, 1105.

  • Serafim, R., de Souza Gama, F. H., Dutra, L. A., Dos Reis, C. V., Vasconcelos, S., da Silva Santiago, A., … Couñago, R. M. (2019). Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2. ACS medicinal chemistry letters, 10(9), 1266–1271.

  • Bushell, S. R., Pike, A. C. W., Falzone, M. E., Rorsman, N. J. G., Ta, C. M., Corey, R. A., … Carpenter, E. P. (2019). The structural basis of lipid scrambling and inactivation in the endoplasmic reticulum scramblase TMEM16K. Nature Communications, 10(1), 3956.

  • Alam, M., Sanchez-Azqueta, A., Janha, O., Flannery, E., Mahindra, A., Mapesa, K., ... Tobin A. (2019). Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science, 365(6456), eaau1682.

  • Schapira, M., Open Lab Notebook Consortium, & Harding, R. J. (2019). Open laboratory notebooks: good for science, good for society, good for scientists. F1000Research, 8, 87.

  • Lepore, R., Kryshtafovych, A., Alahuhta, M., Veraszto, H. A., Bomble, Y. J., Bufton, J. C., … Schwede, T. (2019). Target highlights in CASP13: Experimental target structures through the eyes of their authors. Proteins, 87(12), 1037–1057.

  • Kramer, J., Woltersdorf, S., Duflot, T., Hiesinger, K., Lillich, F., Knöll, F., ... Proschak, E. (2019). Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain. Journal Of Medicinal Chemistry, 62(18), 8443-8460.

  • Asquith, C., Maffuid, K., Laitinen, T., Torrice, C., Tizzard, G., Crona, D., & Zuercher, W. (2019). Targeting an EGFR Water Network with 4‐Anilinoquin(az)oline Inhibitors for Chordoma. Chemmedchem, 14(19), 1693-1700.

  • Schäfer, A., Gjerga, E., Welford, R. W., Renz, I., Lehembre, F., Groenen, P. M., … Gstaiger, M. (2019). Elucidating essential kinases of endothelin signalling by logic modelling of phosphoproteomics data. Molecular systems biology, 15(8), e8828.

  • Taylor, A., Swewczyk, M., Kennedy, S., Trush, V., Wu, H., Zeng, H., ... Owen, D. (2019). Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3–9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase. Journal Of Medicinal Chemistry, 62(17), 7669-7683.

  • Fong, J., Pignata, L., Goy, P., Kawabata, K., Lee, S., Koh, C., ... Guccione, E. (2019). Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation. Cancer Cell, 36(2), 194-209.e9.

  • Kaustov, L., Lemak, A., Wu, H., Faini, M., Fan, L., Fang, X., … Arrowsmith, C. H. (2019). The MLL1 trimeric catalytic complex is a dynamic conformational ensemble stabilized by multiple weak interactions. Nucleic acids research, 47(17), 9433–9447.

  • Lei, M., Tempel, W., Chen, S., Liu, K., & Min, J. (2019). Plasticity at the DNA recognition site of the MeCP2 mCG-binding domain. Biochimica Et Biophysica Acta (BBA) - Gene Regulatory Mechanisms, 1862(9), 194409.

  • Abdul Azeez, K. R., Chatterjee, S., Yu, C., Golub, T. R., Sobott, F., & Elkins, J. M. (2019). Structural mechanism of synergistic activation of Aurora kinase B/C by phosphorylated INCENP. Nature communications, 10(1), 3166.

  • Amon, S., Meier-Abt, F., Gillet, L. C., Dimitrieva, S., Theocharides, A., Manz, M. G., & Aebersold, R. (2019). Sensitive Quantitative Proteomics of Human Hematopoietic Stem and Progenitor Cells by Data-independent Acquisition Mass Spectrometry. Molecular & cellular proteomics : MCP, 18(7), 1454–1467.

  • Zhu, D., Huang, H., Pinkas, D. M., Luo, J., Ganguly, D., Fox, A. E., … Lu, X. (2019). 2-Amino-2,3-dihydro-1H-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy. Journal of medicinal chemistry, 62(16), 7431–7444.

  • Asquith, C., Treiber, D., & Zuercher, W. (2019). Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK). Bioorganic & Medicinal Chemistry Letters, 29(14), 1727-1731.

  • Mader, P., Mendoza-Sanchez, R., Iqbal, A., Dong, A., Dobrovetsky, E., Corless, V., ... Arrowsmith, C. (2019). Identification and characterization of the first fragment hits for SETDB1 Tudor domain. Bioorganic & Medicinal Chemistry, 27(17), 3866-3878.

  • Zhang, C., Creech, K. L., Zuercher, W. J., & Willson, T. M. (2019). Gram-scale synthesis of FICZ, a photoreactive endogenous ligand of the aryl hydrocarbon receptor. Scientific reports, 9(1), 9982.

  • Asquith, C., Fleck, N., Torrice, C., Crona, D., Grundner, C., & Zuercher, W. (2019). Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines. Bioorganic & Medicinal Chemistry Letters, 29(18), 2695-2699.

  • Böttcher, J., Dilworth, D., Reiser, U., Neumüller, R., Schleicher, M., Petronczki, M., ... McConnell D. (2019). Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nature Chemical Biology, 15(8), 822-829.

  • Chen, S., Zhang, W., Min, J., & Liu, K. (2019). Lesson from a Fab-enabled co-crystallization study of TDRD2 and PIWIL1. Methods.

  • Mathea, S., Salah, E., & Knapp, S. (2019). High-Throughput Purification of Protein Kinases from Escherichia coli and Insect Cells. Methods In Molecular Biology, 191-202.

  • Chen, Z., Picaud, S., Filippakopoulos, P., D'Angiolella, V., & Bullock, A. N. (2019). Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase. Structure (London, England : 1993), 27(9), 1395–1404.e4.

  • Carter, A., Kraemer, O., Zwick, M., Mueller-Fahrnow, A., Arrowsmith, C., & Edwards, A. (2019). Target 2035: probing the human proteome. Drug Discovery Today, 24(11), 2111-2115.

  • Xiong, Y., Greschik, H., Johansson, C., Seifert, L., Bacher, J., Park, K, ... Jin J. (2019). Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). Journal Of Medicinal Chemistry, 62(20), 8996-9007.

  • Fang, H., De Wolf, H., Knezevic, B., Burnham, K., Osgood, J., Sanniti, A., ... Knight, J. (2019). A genetics-led approach defines the drug target landscape of 30 immune-related traits. Nature Genetics, 51(7), 1082-1091.

  • Halabelian, L., Ravichandran, M., Li, Y., Zeng, H., Rao, A., Aravind, L., & Arrowsmith, C. H. (2019). Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition. Nature structural & molecular biology, 26(7), 607–612.

  • Thomas, S. E., Collins, P., James, R. H., Mendes, V., Charoensutthivarakul, S., Radoux, C., … Blundell, T. L. (2019). Structure-guided fragment-based drug discovery at the synchrotron: screening binding sites and correlations with hotspot mapping. Philosophical transactions. Series A, Mathematical, physical, and engineering sciences, 377(2147), 20180422.

  • Verdonck, S., Pu, S., Sorrell, F., Elkins, J., Froeyen, M., Gao, L., ...  De Jonghe, S. (2019). Synthesis and Structure–Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3-b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. Journal Of Medicinal Chemistry, 62(12), 5810-5831.

  • Celis-Gutierrez, J., Blattmann, P., Zhai, Y., Jarmuzynski, N., Ruminski, K., Grégoire, C., … Malissen, B. (2019). Quantitative Interactomics in Primary T Cells Provides a Rationale for Concomitant PD-1 and BTLA Coinhibitor Blockade in Cancer Immunotherapy. Cell reports, 27(11), 3315–3330.e7.

  • Bergqvist, F., Ossipova, E., Idborg, H., Raouf, J., Checa, A., Englund, K., ... Jakobsson, P. J. (2019). Inhibition of mPGES-1 or COX-2 Results in Different Proteomic and Lipidomic Profiles in A549 Lung Cancer Cells. Frontiers in pharmacology, 10, 636.

  • Resnick, E., Bradley, A., Gan, J., Douangamath, A., Krojer, T., Sethi, R., … London, N. (2019). Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. Journal of the American Chemical Society, 141(22), 8951–8968.

  • Dilworth, D., Barsyte-Lovejoy, D. (2019). Targeting protein methylation: from chemical tools to precision medicines. Cellular And Molecular Life Sciences, 76(15), 2967-2985.

  • Fox, N. G., Yu, X., Feng, X., Bailey, H. J., Martelli, A., Nabhan, J. F., … Han, S. (2019). Structure of the human frataxin-bound iron-sulfur cluster assembly complex provides insight into its activation mechanism. Nature communications, 10(1), 2210.

  • Idborg, H., Zandian, A., Ossipova, E., Wigren, E., Preger, C., Mobarrez, F., ... Jakobsson, P. J. (2019). Circulating Levels of Interferon Regulatory Factor-5 Associates With Subgroups of Systemic Lupus Erythematosus Patients. Frontiers in immunology, 10, 1029.

  • Le Bihan, Y. V., Lanigan, R. M., Atrash, B., McLaughlin, M. G., Velupillai, S., Malcolm, A. G., … Bavetsias, V. (2019). C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. European journal of medicinal chemistry, 177, 316–337.

  • Chen, S., Wiewiora, R. P., Meng, F., Babault, N., Ma, A., Yu, W., … Luo, M. (2019). The dynamic conformational landscape of the protein methyltransferase SETD8. eLife, 8, e45403.

  • Carvalho, D., Taylor, K., Olaciregui, N., Molinari, V., Clarke, M., Mackay, A., ... Jones, C., (2019). ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Communications Biology, 2(1).

  • Drewry, D., Wells, C., Zuercher, W., & Willson, T. (2019). A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction. SLAS Discovery: Advancing Life Sciences R&D, 24(5), 505-514.

  • Zhang, R., McIntyre, P., Collins, P., Foley, D., Arter, C., von Delft, F., ... Nelson, A. (2019). Construction of a Shape‐Diverse Fragment Set: Design, Synthesis and Screen against Aurora‐A Kinase. Chemistry – A European Journal, 25(27), 6831-6839.

  • Wang, J., Varin, T., Vieth, M., & Elkins, J. M. (2019). Crystal structure of human RIOK2 bound to a specific inhibitor. Open biology, 9(4), 190037.

  • Suh, J. L., Barnash, K. D., Abramyan, T. M., Li, F., The, J., Engelberg, I. A., … Frye, S. V. (2019). Discovery of selective activators of PRC2 mutant EED-I363M. Scientific reports, 9(1), 6524.

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