Publications

2021

Santhakumar, V., Sutherland, M., Li, A., Kaghad, A., Panagopoulos, D., Li, F., Szewczyk, M., Smil, D., Scholten, C., Bouché, L., Stellfeld, T., Arrowsmith, C. H., Barsyte, D., Vedadi, M., Hartung, I. V., Steuber, H., & Britton, R. (2021). Rational Design and Synthesis of Selective PRMT4 Inhibitors: a New Chemotype for Development of Cancer Therapeutics. ChemMedChem, 10.1002/cmdc.202100018. Advance online publication. https://doi.org/10.1002/cmdc.202100018

Williams, E., Riesebos, E., Kerr, G., & Bullock, A. N. (2021). ALK2 Receptor Kinase Association with FKBP12.6 Is Structurally Conserved with the ALK2-FKBP12 Complex. Biomedicines, 9(2), 129. https://doi.org/10.3390/biomedicines9020129

Lemos, C., Schulze, V. K., Baumgart, S. J., Nevedomskaya, E., Heinrich, T., Lefranc, J., Bader, B., Christ, C. D., Briem, H., Kuhnke, L. P., Holton, S. J., Bömer, U., Lienau, P., von Nussbaum, F., Nising, C. F., Bauser, M., Hägebarth, A., Mumberg, D., & Haendler, B. (2021). The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models. Cellular oncology (Dordrecht), 10.1007/s13402-020-00584-8. Advance online publication. https://doi.org/10.1007/s13402-020-00584-8

Berger, B. T., Amaral, M., Kokh, D. B., Nunes-Alves, A., Musil, D., Heinrich, T., Schröder, M., Neil, R., Wang, J., Navratilova, I., Bomke, J., Elkins, J. M., Müller, S., Frech, M., Wade, R. C., & Knapp, S. (2021). Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2. Cell chemical biology, S2451-9456(21)00003-9. Advance online publication. https://doi.org/10.1016/j.chembiol.2021.01.003

D'Amico, F., Mukhopadhyay, R., Ovaa, H., & Mulder, M. (2021). Targeting TRIM Proteins: A quest towards drugging an emerging protein class. Chembiochem : a European journal of chemical biology, 10.1002/cbic.202000787. Advance online publication. https://doi.org/10.1002/cbic.202000787

Wells, C. I., Al-Ali, H., Andrews, D. M., Asquith, C., Axtman, A. D., Dikic, I., Ebner, D., Ettmayer, P., Fischer, C., Frederiksen, M., Futrell, R. E., Gray, N. S., Hatch, S. B., Knapp, S., Lücking, U., Michaelides, M., Mills, C. E., Müller, S., Owen, D., Picado, A., … Drewry, D. H. (2021). The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. International journal of molecular sciences, 22(2), 566. https://doi.org/10.3390/ijms22020566

2020

Forster, M., Liang, X. J., Schröder, M., Gerstenecker, S., Chaikuad, A., Knapp, S., Laufer, S., & Gehringer, M. (2020). Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK. International journal of molecular sciences, 21(23), 9269. https://doi.org/10.3390/ijms21239269

Ramachandran, S., & Ciulli, A. (2020). Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues. Current opinion in structural biology, 67, 110–119. Advance online publication. https://doi.org/10.1016/j.sbi.2020.10.009

Ishida, T., & Ciulli, A. (2020). E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones. SLAS discovery : advancing life sciences R & D, 2472555220965528. Advance online publication. https://doi.org/10.1177/2472555220965528

Preuss, F., Chatterjee, D., Mathea, S., Shrestha, S., St-Germain, J., Saha, M., Kannan, N., Raught, B., Rottapel, R., & Knapp, S. (2020). Nucleotide Binding, Evolutionary Insights, and Interaction Partners of the Pseudokinase Unc-51-like Kinase 4. Structure (London, England : 1993), 28(11), 1184–1196.e6. https://doi.org/10.1016/j.str.2020.07.016

Schröder, M., Bullock, A. N., Fedorov, O., Bracher, F., Chaikuad, A., & Knapp, S. (2020). DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity. Journal of medicinal chemistry, 63(18), 10224–10234. https://doi.org/10.1021/acs.jmedchem.0c00898

Wu, Q., Ba-Alawi, W., Deblois, G., Cruickshank, J., Duan, S., Lima-Fernandes, E., Haight, J., Tonekaboni, S., Fortier, A. M., Kuasne, H., McKee, T. D., Mahmoud, H., Kushida, M., Cameron, S., Dogan-Artun, N., Chen, W., Nie, Y., Zhang, L. X., Vellanki, R. N., Zhou, S., … Arrowsmith, C. H. (2020). GLUT1 inhibition blocks growth of RB1-positive triple negative breast cancer. Nature communications, 11(1), 4205. https://doi.org/10.1038/s41467-020-18020-8