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X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.

Abstract:

The protein kinase ERK5 (MAPK7) is an emerging drug target for a variety of indications, in particular for cancer where it plays a key role mediating cell proliferation, survival, epithelial-mesenchymal transition, and angiogenesis. To date, no three-dimensional structure has been published that would allow rational design of inhibitors. To address this, we determined the X-ray crystal structure of the human ERK5 kinase domain in complex with a highly specific benzo[e]pyrimido[5,4-b]diazepine...

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Publication status:
Published

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Publisher copy:
10.1021/jm4000837

Authors


Elkins, JM More by this author
Pattison, MJ More by this author
Arthur, JS More by this author
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Journal:
Journal of medicinal chemistry
Volume:
56
Issue:
11
Pages:
4413-4421
Publication date:
2013-06-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:aff99b9b-e079-40bd-ba8f-7f666f28581f
Source identifiers:
401244
Local pid:
pubs:401244

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