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Selective JAK3 inhibitors with a covalent reversible binding mode targeting a new induced fit binding pocket

Abstract:

Janus kinases (JAKs) are a family of cytoplasmatic tyrosine kinases that are attractive targets for the development of anti-inflammatory drugs given their roles in cytokine signaling. One question regarding JAKs and their inhibitors that remains under intensive debate is whether JAK inhibitors should be isoform selective. Since JAK3 functions are restricted to immune cells, an isoform-selective inhibitor for JAK3 could be especially valuable to achieve clinically more useful and precise effec...

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

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Publisher copy:
10.1016/j.chembiol.2016.10.008

Authors


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Bayer Pharma AG More from this funder
Boehringer Ingelheim More from this funder
Canada Foundation for Innovation More from this funder
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Publisher:
Elsevier Publisher's website
Journal:
Cell Chemical Biology Journal website
Volume:
23
Issue:
11
Pages:
1335-1340
Publication date:
2018-11-10
Acceptance date:
2018-10-13
DOI:
EISSN:
2451-9456
ISSN:
2451-9456
Pubs id:
pubs:660324
URN:
uri:5f6fb850-fb14-4027-9bc8-66970ffa90c9
UUID:
uuid:5f6fb850-fb14-4027-9bc8-66970ffa90c9
Local pid:
pubs:660324

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