| Publikationstyp: | Beitrag in wissenschaftlicher Zeitschrift |
| Art der Begutachtung: | Peer review (Publikation) |
| Titel: | Targeted polypharmacology : discovery of a highly potent non-hydroxamate dual matrix metalloproteinase (MMP)-10/-13 inhibitor |
| Autor/-in: | Senn, Nicole Ott, Michael Lanz, Jan Riedl, Rainer |
| DOI: | 10.1021/acs.jmedchem.7b01001 |
| Erschienen in: | Journal of Medicinal Chemistry |
| Band(Heft): | 60 |
| Heft: | 23 |
| Seite(n): | 9585 |
| Seiten bis: | 9598 |
| Erscheinungsdatum: | 2017 |
| Verlag / Hrsg. Institution: | American Chemical Society |
| ISSN: | 0022-2623 |
| Sprache: | Englisch |
| Schlagwörter: | Drug design; Humans; Matrix metalloproteinase 10; Matrix metalloproteinase 13; Matrix metalloproteinase inhibitors; Molecular models; Polypharmacology; Structure-activity relationship |
| Fachgebiet (DDC): | 572: Biochemie 615: Pharmakologie und Therapeutik |
| Zusammenfassung: | Matrix metalloproteinases (MMPs) play a key role in many diseases like cancer, atherosclerosis or arthritis. Interest in MMP inhibition has been revitalized very recently as the knowledge on the underlying network of biological pathways is steadily growing. On the basis of this new insight into the relevance of MMP-10 and MMP-13 within the MMP network and the ban of hydroxamate inhibitors from clinical development, the discovery of non-hydroxamate multitarget drugs against specific MMPs is of foremost interest. Here, we disclose the discovery of a very potent and selective non-hydroxamate MMP-10/-13 inhibitor. The high potency (IC50of 31 nM [MMP-10] and 5 nM [MMP-13]) and selectivity over MMP-1, -2, -3, -7, -8, -9, -12, and -14 enable this compound to decipher disease causing MMP networks and to generate new treatment options through targeted polypharmacology. |
| URI: | https://digitalcollection.zhaw.ch/handle/11475/2915 |
| Volltext Version: | Publizierte Version |
| Lizenz (gemäss Verlagsvertrag): | Lizenz gemäss Verlagsvertrag |
| Departement: | Life Sciences und Facility Management |
| Enthalten in den Sammlungen: | Publikationen Life Sciences und Facility Management |
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Senn, N., Ott, M., Lanz, J., & Riedl, R. (2017). Targeted polypharmacology : discovery of a highly potent non-hydroxamate dual matrix metalloproteinase (MMP)-10/-13 inhibitor. Journal of Medicinal Chemistry, 60(23), 9585–9598. https://doi.org/10.1021/acs.jmedchem.7b01001
Senn, N. et al. (2017) ‘Targeted polypharmacology : discovery of a highly potent non-hydroxamate dual matrix metalloproteinase (MMP)-10/-13 inhibitor’, Journal of Medicinal Chemistry, 60(23), pp. 9585–9598. Available at: https://doi.org/10.1021/acs.jmedchem.7b01001.
N. Senn, M. Ott, J. Lanz, and R. Riedl, “Targeted polypharmacology : discovery of a highly potent non-hydroxamate dual matrix metalloproteinase (MMP)-10/-13 inhibitor,” Journal of Medicinal Chemistry, vol. 60, no. 23, pp. 9585–9598, 2017, doi: 10.1021/acs.jmedchem.7b01001.
SENN, Nicole, Michael OTT, Jan LANZ und Rainer RIEDL, 2017. Targeted polypharmacology : discovery of a highly potent non-hydroxamate dual matrix metalloproteinase (MMP)-10/-13 inhibitor. Journal of Medicinal Chemistry. 2017. Bd. 60, Nr. 23, S. 9585–9598. DOI 10.1021/acs.jmedchem.7b01001
Senn, Nicole, Michael Ott, Jan Lanz, and Rainer Riedl. 2017. “Targeted Polypharmacology : Discovery of a Highly Potent Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-10/-13 Inhibitor.” Journal of Medicinal Chemistry 60 (23): 9585–98. https://doi.org/10.1021/acs.jmedchem.7b01001.
Senn, Nicole, et al. “Targeted Polypharmacology : Discovery of a Highly Potent Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-10/-13 Inhibitor.” Journal of Medicinal Chemistry, vol. 60, no. 23, 2017, pp. 9585–98, https://doi.org/10.1021/acs.jmedchem.7b01001.
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