A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus
Systemic lupus erythematosus is a chronic inflammatory disease, in which treatment is still limited due to suboptimal efficacy and toxicities associated with the available therapies. JAK kinases are well known to play an important role in systemic lupus erythematous. There is growing evidence that R...
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Elsevier
2021-04-01
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| Series: | Journal of Pharmacological Sciences |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S134786132100013X |
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doaj-68149f6ba7294e63ad8e5e6d2edd988c2021-03-11T04:24:11ZengElsevierJournal of Pharmacological Sciences1347-86132021-04-011454340348A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosusMaria Dulak-Lis0Anna Bujak1Kamila Gala2Martyna Banach3Urszula Kędzierska4Joanna Miszkiel5Joanna Hucz-Kalitowska6Michał Mroczkiewicz7Bartosz Stypik8Krzysztof Szymczak9Paweł Gunerka10Krzysztof Dubiel11Beata M. Zygmunt12Maciej Wieczorek13Jerzy S. Pieczykolan14Celon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, Poland; Corresponding author.Celon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandCelon Pharma S.A., Preclinical Department, Mokra 41a, Kiełpin, 05-092, Łomianki, PolandSystemic lupus erythematosus is a chronic inflammatory disease, in which treatment is still limited due to suboptimal efficacy and toxicities associated with the available therapies. JAK kinases are well known to play an important role in systemic lupus erythematous. There is growing evidence that ROCK kinases are also important in disease development. In this paper, we present the results of the development of CPL409116, a dual JAK and ROCK inhibitor. The studies we performed demonstrate that this molecule is an effective JAK and ROCK inhibitor which efficiently blocks disease progression in NZBWF1/J mouse models of systemic lupus erythematous.http://www.sciencedirect.com/science/article/pii/S134786132100013XJAK3JAK1LupusROCKNephritis |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Maria Dulak-Lis Anna Bujak Kamila Gala Martyna Banach Urszula Kędzierska Joanna Miszkiel Joanna Hucz-Kalitowska Michał Mroczkiewicz Bartosz Stypik Krzysztof Szymczak Paweł Gunerka Krzysztof Dubiel Beata M. Zygmunt Maciej Wieczorek Jerzy S. Pieczykolan |
| spellingShingle |
Maria Dulak-Lis Anna Bujak Kamila Gala Martyna Banach Urszula Kędzierska Joanna Miszkiel Joanna Hucz-Kalitowska Michał Mroczkiewicz Bartosz Stypik Krzysztof Szymczak Paweł Gunerka Krzysztof Dubiel Beata M. Zygmunt Maciej Wieczorek Jerzy S. Pieczykolan A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus Journal of Pharmacological Sciences JAK3 JAK1 Lupus ROCK Nephritis |
| author_facet |
Maria Dulak-Lis Anna Bujak Kamila Gala Martyna Banach Urszula Kędzierska Joanna Miszkiel Joanna Hucz-Kalitowska Michał Mroczkiewicz Bartosz Stypik Krzysztof Szymczak Paweł Gunerka Krzysztof Dubiel Beata M. Zygmunt Maciej Wieczorek Jerzy S. Pieczykolan |
| author_sort |
Maria Dulak-Lis |
| title |
A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus |
| title_short |
A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus |
| title_full |
A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus |
| title_fullStr |
A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus |
| title_full_unstemmed |
A novel JAK/ROCK inhibitor, CPL409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus |
| title_sort |
novel jak/rock inhibitor, cpl409116, demonstrates potent efficacy in the mouse model of systemic lupus erythematosus |
| publisher |
Elsevier |
| series |
Journal of Pharmacological Sciences |
| issn |
1347-8613 |
| publishDate |
2021-04-01 |
| description |
Systemic lupus erythematosus is a chronic inflammatory disease, in which treatment is still limited due to suboptimal efficacy and toxicities associated with the available therapies. JAK kinases are well known to play an important role in systemic lupus erythematous. There is growing evidence that ROCK kinases are also important in disease development. In this paper, we present the results of the development of CPL409116, a dual JAK and ROCK inhibitor. The studies we performed demonstrate that this molecule is an effective JAK and ROCK inhibitor which efficiently blocks disease progression in NZBWF1/J mouse models of systemic lupus erythematous. |
| topic |
JAK3 JAK1 Lupus ROCK Nephritis |
| url |
http://www.sciencedirect.com/science/article/pii/S134786132100013X |
| work_keys_str_mv |
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