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Structural analysis of inhibitor binding to CAMKK1 identifies features necessary for design of specific inhibitors

Abstract:

The calcium/calmodulin-dependent protein kinases (CAMKKs) are upstream activators of CAMK1 and CAMK4 signalling and have important functions in neural development, maintenance and signalling, as well as in other aspects of biology such as Ca2+ signalling in the cardiovascular system. To support the development of specific inhibitors of CAMKKs we have determined the crystal structure of CAMKK1 with two ATP-competitive inhibitors. The structures reveal small but exploitable differences between ...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1038/s41598-018-33043-4

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Role:
Author
ORCID:
0000-0002-3973-3370
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Role:
Author
ORCID:
0000-0001-6716-2504
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São Paulo Research Foundation More from this funder
Brazilian National Council for Scientific and Technological Development More from this funder
Brazilian Coordination for the Improvement of Higher Education Personnel More from this funder
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Publisher:
Nature Publishing Group Publisher's website
Journal:
Scientific Reports Journal website
Volume:
8
Issue:
1
Pages:
14800
Publication date:
2018-10-04
Acceptance date:
2018-09-18
DOI:
EISSN:
2045-2322
Pubs id:
pubs:927567
URN:
uri:c4652b52-acfb-4938-89f6-a2d3597671e8
UUID:
uuid:c4652b52-acfb-4938-89f6-a2d3597671e8
Local pid:
pubs:927567
Language:
English
Keywords:

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