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.
Publications
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 communications, 12(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.
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.
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.
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. eLife, 9, 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.
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.
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.
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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