Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8

Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.

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Bibliographische Detailangaben
Veröffentlicht in:	ACS medicinal chemistry letters 2016-06, Vol.7 (6), p.595-600
Hauptverfasser:	Bergeron, Philippe, Koehler, Michael F. T, Blackwood, Elizabeth M, Bowman, Krista, Clark, Kevin, Firestein, Ron, Kiefer, James R, Maskos, Klaus, McCleland, Mark L, Orren, Linda, Ramaswamy, Sreemathy, Salphati, Laurent, Schmidt, Steve, Schneider, Elisabeth V, Wu, Jiansheng, Beresini, Maureen
Format:	Artikel
Sprache:	eng
Schlagworte:	Letter
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Beschreibung
Zusammenfassung:	Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.
ISSN:	1948-5875 1948-5875
DOI:	10.1021/acsmedchemlett.6b00044