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Titel:

Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1)

Dokumenttyp:
Zeitschriftenaufsatz
Autor(en):
Ostrovskyi, Dmytro; Rumpf, Tobias; Eib, Julia; Lumbroso, Alexandre; Slynko, Inna; Klaeger, Susan; Heinzlmeir, Stephanie; Forster, Michael; Gehringer, Matthias; Pfaffenrot, Ellen; Bauer, Silke Mona; Schmidtkunz, Karin; Wenzler, Sandra; Metzger, Eric; Kuster, Bernhard; Laufer, Stefan; Schüle, Roland; Sippl, Wolfgang; Breit, Bernhard; Jung, Manfred
Abstract:
AIM: The histone kinase PRK1 has been identified as a potential target to combat prostate cancer but selective PRK1 inhibitors are lacking. The US FDA -approved JAK1-3 inhibitor tofacitinib also potently inhibits PRK1 in vitro. RESULTS: We show that tofacitinib also inhibits PRK1 in a cellular setting. Using tofacitinib as a starting point for structure-activity relationship studies, we identified a more potent and another more selective PRK1 inhibitor compared with tofacitinib. Furthermore, we...     »
Stichworte:
BayBioMS
Zeitschriftentitel:
Future Medicinal Chemistry
Jahr:
2016
Band / Volume:
8
Heft / Issue:
13
Seitenangaben Beitrag:
1537-1551
Volltext / DOI:
doi:10.4155/fmc-2016-0132
Verlag / Institution:
Future Science, LTD
E-ISSN:
1756-89191756-8927
Publikationsdatum:
01.09.2016
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