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A chemical proteomic strategy reveals inhibitors of lipoate salvage in bacteria and parasites
Dienemann, J. N., Chen, S. Y., Hitzenberger, M., Sievert, M. L., Hacker, S. M., Prigge, S. T., … Sieber, S. A. (2023). A chemical proteomic strategy reveals inhibitors of lipoate salvage in bacteria and parasites. Angewandte Chemie International Edition, 62(31), e202304533 (9 pp.). https://doi.org/10.1002/anie.202304533
Chemistry-led investigations into the mode of action of NAMPT activators, resulting in the discovery of non-pyridyl class NAMPT activators
Tang, S., Garzon Sanz, M., Smith, O., Krämer, A., Egbase, D., Caton, P. W., … Butterworth, S. (2023). Chemistry-led investigations into the mode of action of NAMPT activators, resulting in the discovery of non-pyridyl class NAMPT activators. Acta Pharmaceutica Sinica B, 13(2), 709-721. https://doi.org/10.1016/j.apsb.2022.07.016
Design and synthesis of tranylcypromine-derived LSD1 inhibitors with improved hERG and microsomal stability profiles
Koda, Y., Sato, S., Yamamoto, H., Niwa, H., Watanabe, H., Watanabe, C., … Umehara, T. (2022). Design and synthesis of tranylcypromine-derived LSD1 inhibitors with improved hERG and microsomal stability profiles. ACS Medicinal Chemistry Letters, 13(5), 848-854. https://doi.org/10.1021/acsmedchemlett.2c00120
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models
Menna, M., Fiorentino, F., Marrocco, B., Lucidi, A., Tomassi, S., Cilli, D., … Mai, A. (2022). Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. European Journal of Medicinal Chemistry, 237, 114410 (23 pp.). https://doi.org/10.1016/j.ejmech.2022.114410
Targeting virulence regulation to disarm <em>Acinetobacter baumannii</em> pathogenesis
Trebosc, V., Lucchini, V., Narwal, M., Wicki, B., Gartenmann, S., Schellhorn, B., … Pieren, M. (2022). Targeting virulence regulation to disarm Acinetobacter baumannii pathogenesis. Virulence, 13(1), 1868-1883. https://doi.org/10.1080/21505594.2022.2135273
Fragment-based discovery of non-bisphosphonate binders of <em>Trypanosoma brucei</em> farnesyl pyrophosphate synthase
Münzker, L., Petrick, J. K., Schleberger, C., Clavel, D., Cornaciu, I., Wilcken, R., … Jahnke, W. (2020). Fragment-based discovery of non-bisphosphonate binders of Trypanosoma brucei farnesyl pyrophosphate synthase. ChemBioChem, 21(21), 3096-3111. https://doi.org/10.1002/cbic.202000246
Locking mixed-lineage kinase domain-like protein in its auto-inhibited state prevents necroptosis
Rübbelke, M., Fiegen, D., Bauer, M., Binder, F., Hamilton, J., King, J., … Zeeb, M. (2020). Locking mixed-lineage kinase domain-like protein in its auto-inhibited state prevents necroptosis. Proceedings of the National Academy of Sciences of the United States of America PNAS, 117(52), 33272-33281. https://doi.org/10.1073/pnas.2017406117
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases
Schubart, A., Anderson, K., Mainolfi, N., Sellner, H., Ehara, T., Adams, C. M., … Eder, J. (2019). Small-molecule factor B inhibitor for the treatment of complement-mediated diseases. Proceedings of the National Academy of Sciences of the United States of America PNAS, 116(16), 7926-7931. https://doi.org/10.1073/pnas.1820892116
Inhibition of 14-3-3/Tau by hybrid small-molecule peptides operating via two different binding modes
Andrei, S. A., Meijer, F. A., Neves, J. F., Brunsveld, L., Landrieu, I., Ottmann, C., & Milroy, L. G. (2018). Inhibition of 14-3-3/Tau by hybrid small-molecule peptides operating via two different binding modes. ACS Chemical Neuroscience, 9(11), 2639-2654. https://doi.org/10.1021/acschemneuro.8b00118
Ligand channel in pharmacologically stabilized rhodopsin
Mattle, D., Kuhn, B., Aebi, J., Bedoucha, M., Kekilli, D., Grozinger, N., … Dawson, R. J. P. (2018). Ligand channel in pharmacologically stabilized rhodopsin. Proceedings of the National Academy of Sciences of the United States of America PNAS, 115(14), 3640-3645. https://doi.org/10.1073/pnas.1718084115
The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer&#039;s disease
Neumann, U., Ufer, M., Jacobson, L. H., Rouzade-Dominguez, M. L., Huledal, G., Kolly, C., … Lopez Lopez, C. (2018). The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease. EMBO Molecular Medicine, 10(11), e9316 (18 pp.). https://doi.org/10.15252/emmm.201809316
Chemoproteomics-aided medicinal chemistry for the discovery of EPHA2 inhibitors
Heinzlmeir, S., Lohse, J., Treiber, T., Kudlinzki, D., Linhard, V., Gande, S. L., … Médard, G. (2017). Chemoproteomics-aided medicinal chemistry for the discovery of EPHA2 inhibitors. ChemMedChem, 12(12), 999-1011. https://doi.org/10.1002/cmdc.201700217
Beyond the BET family: targeting CBP/p300 with 4-acyl pyrroles
Hügle, M., Lucas, X., Ostrovskyi, D., Regenass, P., Gerhardt, S., Einsle, O., … Wohlwend, D. (2017). Beyond the BET family: targeting CBP/p300 with 4-acyl pyrroles. Angewandte Chemie International Edition, 56(41), 12476-12480. https://doi.org/10.1002/anie.201705516
Mechanism-based inhibitors of the human sirtuin 5 deacylase: structure–activity relationship, biostructural, and kinetic insight
Rajabi, N., Auth, M., Troelsen, K. R., Pannek, M., Bhatt, D. P., Fontenas, M., … Olsen, C. A. (2017). Mechanism-based inhibitors of the human sirtuin 5 deacylase: structure–activity relationship, biostructural, and kinetic insight. Angewandte Chemie International Edition, 56(47), 14836-14841. https://doi.org/10.1002/anie.201709050
Insight into the Inhibition of drug-resistant mutants of the receptor tyrosine kinase EGFR
Engel, J., Becker, C., Lategahn, J., Keul, M., Ketzer, J., Mühlenberg, T., … Rauh, D. (2016). Insight into the Inhibition of drug-resistant mutants of the receptor tyrosine kinase EGFR. Angewandte Chemie International Edition, 55(36), 10909-10912. https://doi.org/10.1002/anie.201605011
Identification of a β1/β2-specific sulfonamide proteasome ligand by crystallographic screening
Beck, P., Reboud-Ravaux, M., & Groll, M. (2015). Identification of a β1/β2-specific sulfonamide proteasome ligand by crystallographic screening. Angewandte Chemie International Edition, 54(38), 11275-11278. https://doi.org/10.1002/anie.201505054
Indolo-phakellins as beta 5-specific noncovalent proteasome inhibitors
Beck, P., Lansdell, T. A., Hewlett, N. M., Tepe, J. J., & Groll, M. (2015). Indolo-phakellins as beta 5-specific noncovalent proteasome inhibitors. Angewandte Chemie International Edition, 54(9), 2830-2833. https://doi.org/10.1002/anie.201410168
Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)
Pomplun, S., Wang, Y., Kirschner, A., Kozany, C., Bracher, A., & Hausch, F. (2015). Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs). Angewandte Chemie International Edition, 54(1), 345-348. https://doi.org/10.1002/ANIE.201408776
Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4
Schröder, P., Förster, T., Kleine, S., Becker, C., Richters, A., Ziegler, S., … Waldmann, H. (2015). Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4. Angewandte Chemie International Edition, 54(42), 12398-12403. https://doi.org/10.1002/anie.201501515
Pseudilins: Halogenated, allosteric inhibitors of the non-mevalonate pathway enzyme IspD
Kunfermann, A., Witschel, M., Illarionov, B., Martin, R., Rottmann, M., Höffken, H. W., … Diederich, F. (2014). Pseudilins: Halogenated, allosteric inhibitors of the non-mevalonate pathway enzyme IspD. Angewandte Chemie International Edition, 53(8), 2235-2239. https://doi.org/10.1002/anie.201309557