Antibiotics

The picture shows interactions between a ligand and its target.

Our group focuses on hit identification and lead development in drug discovery. We work on targets of importance in infectious diseases with a focus on Gram-Negative infections, Tuberculosis and Malaria. In this work we are integrating computational medicinal chemistry tools with organic chemistry. We work in close collaboration with microbiologists, biochemists and structural biologists.

Contact Anders Karlén

Publications

Novel Allosteric Mechanism of Dual p53/MDM2 and p53/MDM4 Inhibition by a Small Molecule.
Grinkevich, V., Vema, A., Fawkner, K., Issaeva, N., Andreotti, V. et al. (2022). Frontiers in Molecular Biosciences, . vol. 9 DOI
Bacterial type I signal peptidase inhibitors-Optimized hits from nature.
Szalaj, N., Benediktsdottir, A., Rusin, D., Karlén, A., Mowbray, S. et al. (2022). European Journal of Medicinal Chemistry, . vol. 238 DOI
Towards the sustainable discovery and development of new antibiotics.
Miethke, M., Pieroni, M., Weber, T., Brönstrup, M., Hammann, P. et al. (2021). Nature Reviews Chemistry, . vol. 5, ss. 726-749 DOI
Antibacterial sulfonimidamide-based oligopeptides as type I signal peptidase inhibitors: Synthesis and biological evaluation.
Benediktsdottir, A., Lu, L., Cao, S., Zamaratski, E., Karlén, A. et al. (2021). European Journal of Medicinal Chemistry, . vol. 224 DOI
ENABLE: an engine for European antibacterial drug discovery and development.
Olliver, M., Griestop, L., Hughes, D., Belfrage, A., Gising, J. et al. (2021). Nature reviews. Drug discovery, vol. 20, ss. 407-408 DOI
Computational studies of molecular pre-organization through macrocyclization: Conformational distribution analysis of closely related non-macrocyclic and macrocyclic analogs.
Olanders, G., Brandt, P., Sköld, C., Karlen, A. (2021). Bioorganic & Medicinal Chemistry, . vol. 49 DOI
Synthesis and in vitro biological evaluation of quinolinyl pyrimidines targeting type II NADH-dehydrogenase (NDH-2).
Lu, L., Åkerbladh, L., Ahmad, S., Konda, V., Cao, S. et al. (2022). ACS Infectious Diseases, . vol. 8, ss. 482-498 DOI
The global preclinical antibacterial pipeline.
Theuretzbacher, U., Outterson, K., Engel, A., Karlen, A. (2020). Nature Reviews Microbiology, vol. 18, ss. 275-285 DOI
Boronic ester-linked macrocyclic lipopeptides as serine protease inhibitors targeting Escherichia coli type I signal peptidase.
Szałaj, N., Lu, L., Benediktsdottir, A., Zamaratski, E., Cao, S. et al. (2018). European Journal of Medicinal Chemistry, vol. 157, ss. 1346-1360 DOI
Conformational Analysis of Macrocycles: Comparing General and Specialized Methods.
Olanders, G., Alogheli, H., Brandt, P., Karlén, A. (2020). Journal of Computer-Aided Molecular Design, vol. 34, ss. 231-252 DOI