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

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

doi:10.1021/acsmedchemlett.6b00044

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

Bergeron, P., Koehler, M. F. T., Blackwood, E. M., Bowman, K., Clark, K., Firestein, R., et al. (2016). Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. ACS Medicinal Chemistry Letters, 7(6), 595-600. doi:10.1021/acsmedchemlett.6b00044.

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Item Permalink: https://hdl.handle.net/11858/00-001M-0000-002B-00F9-F Version Permalink: https://hdl.handle.net/11858/00-001M-0000-002B-00FA-D

Genre: Journal Article

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Creators:
Bergeron, Philippe¹, Author
Koehler, Michael F. T.¹, Author
Blackwood, Elizabeth M.¹, Author
Bowman, Krista¹, Author
Clark, Kevin¹, Author
Firestein, Ron¹, Author
Kiefer, James R.¹, Author
Maskos, Klaus¹, Author
McCleland, Mark L.¹, Author
Orren, Linda¹, Author
Ramaswamy, Sreemathy¹, Author
Salphati, Laurent¹, Author
Schmidt, Steve¹, Author
Schneider, Elisabeth V.², Author
Wu, Jiansheng¹, Author
Beresini, Maureen¹, Author

Affiliations:
1external, ou_persistent22
2Huber, Robert / Structure Research, Max Planck Institute of Biochemistry, Max Planck Society, ou_1565155

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Free keywords: KINASE INHIBITOR; BETA-CATENIN; MEDIATOR COMPLEX; TRANSCRIPTION; CELLSPharmacology & Pharmacy; Sorafenib; CDK8; inhibitor; DMG-out;

Abstract: 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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Language(s): eng - English

Dates: Date issued: 2016

Publication Status: Issued

Pages: 6

Publishing info: -

Table of Contents: -

Rev. Type: Peer

Identifiers: ISI: 000377845200012
DOI: 10.1021/acsmedchemlett.6b00044

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Title: ACS Medicinal Chemistry Letters

Source Genre: Journal

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Publ. Info: Washington, DC : ACS

Pages: - Volume / Issue: 7 (6) Sequence Number: - Start / End Page: 595 - 600 Identifier: Other: 1948-5875
CoNE: https://pure.mpg.de/cone/journals/resource/1948-5875