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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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 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: 2016
 Publication Status: Published in print
 Pages: 6
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Degree: -

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Title: ACS Medicinal Chemistry Letters
Source Genre: Journal
 Creator(s):
Affiliations:
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