| Publikationstyp: | Beitrag in wissenschaftlicher Zeitschrift |
| Art der Begutachtung: | Peer review (Publikation) |
| Titel: | Discovery of a class of potent and selective non‐competitive sentrin‐specific protease 1 inhibitors |
| Autor/-in: | Lindenmann, Urs Brand, Michael Gall, Flavio Frasson, David Hunziker, Lukas Kroslakova, Ivana Sievers, Martin Riedl, Rainer |
| et. al: | No |
| DOI: | 10.1002/cmdc.202000067 |
| Erschienen in: | ChemMedChem |
| Band(Heft): | 15 |
| Heft: | 8 |
| Seite(n): | 675 |
| Seiten bis: | 679 |
| Erscheinungsdatum: | 21-Feb-2020 |
| Verlag / Hrsg. Institution: | Wiley |
| ISSN: | 1860-7179 1860-7187 |
| Sprache: | Englisch |
| Schlagwörter: | Drug design; Drug discovery; Inhibitors; Medicinal chemistry; Structure-activity relationship |
| Fachgebiet (DDC): | 615: Pharmakologie und Therapeutik |
| Zusammenfassung: | Sentrin-specific proteases (SENPs) are responsible for the maturation of small ubiquitin-like modifiers (SUMOs) and the deconjugation of SUMOs from their substrate proteins. Studies on prostate cancer revealed an overexpression of SENP1, which promotes prostate cancer progression as well as metastasis. Therefore, SENP1 has been identified as a novel drug target against prostate cancer. Herein, we report the discovery and biological evaluation of potent and selective SENP1 inhibitors. A structure-activity relationship (SAR) of the newly identified pyridone scaffold revealed allosteric inhibitors with very attractive in vitro ADMET properties regarding plasma binding and plasma stability for this challenging target. This study also emphasizes the importance of biochemical mode of inhibition studies for de novo designed inhibitors. |
| URI: | https://digitalcollection.zhaw.ch/handle/11475/21813 |
| Volltext Version: | Publizierte Version |
| Lizenz (gemäss Verlagsvertrag): | Lizenz gemäss Verlagsvertrag |
| Departement: | Life Sciences und Facility Management |
| Organisationseinheit: | Institut für Chemie und Biotechnologie (ICBT) |
| Enthalten in den Sammlungen: | Publikationen Life Sciences und Facility Management |
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Lindenmann, U., Brand, M., Gall, F., Frasson, D., Hunziker, L., Kroslakova, I., Sievers, M., & Riedl, R. (2020). Discovery of a class of potent and selective non‐competitive sentrin‐specific protease 1 inhibitors. ChemMedChem, 15(8), 675–679. https://doi.org/10.1002/cmdc.202000067
Lindenmann, U. et al. (2020) ‘Discovery of a class of potent and selective non‐competitive sentrin‐specific protease 1 inhibitors’, ChemMedChem, 15(8), pp. 675–679. Available at: https://doi.org/10.1002/cmdc.202000067.
U. Lindenmann et al., “Discovery of a class of potent and selective non‐competitive sentrin‐specific protease 1 inhibitors,” ChemMedChem, vol. 15, no. 8, pp. 675–679, Feb. 2020, doi: 10.1002/cmdc.202000067.
LINDENMANN, Urs, Michael BRAND, Flavio GALL, David FRASSON, Lukas HUNZIKER, Ivana KROSLAKOVA, Martin SIEVERS und Rainer RIEDL, 2020. Discovery of a class of potent and selective non‐competitive sentrin‐specific protease 1 inhibitors. ChemMedChem. 21 Februar 2020. Bd. 15, Nr. 8, S. 675–679. DOI 10.1002/cmdc.202000067
Lindenmann, Urs, Michael Brand, Flavio Gall, David Frasson, Lukas Hunziker, Ivana Kroslakova, Martin Sievers, and Rainer Riedl. 2020. “Discovery of a Class of Potent and Selective Non‐Competitive Sentrin‐Specific Protease 1 Inhibitors.” ChemMedChem 15 (8): 675–79. https://doi.org/10.1002/cmdc.202000067.
Lindenmann, Urs, et al. “Discovery of a Class of Potent and Selective Non‐Competitive Sentrin‐Specific Protease 1 Inhibitors.” ChemMedChem, vol. 15, no. 8, Feb. 2020, pp. 675–79, https://doi.org/10.1002/cmdc.202000067.
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