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Inhibitor‐based affinity probes for the investigation of JAK signaling pathways
Author(s) -
Höfener Michael,
Pachl Fiona,
Kuster Bernhard,
Sewald Norbert
Publication year - 2015
Publication title -
proteomics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.26
H-Index - 167
eISSN - 1615-9861
pISSN - 1615-9853
DOI - 10.1002/pmic.201400324
Subject(s) - janus kinase , kinase , signal transduction , mapk/erk pathway , jak stat signaling pathway , microbiology and biotechnology , computational biology , mitogen activated protein kinase , biology , chemistry , cancer research , receptor tyrosine kinase
The Janus Kinase (JAK) signaling pathway plays a key role for many cellular processes and has recently been correlated with neuronal disorders. In order to understand new links of JAK family members with other signaling pathways, chemical proteomics tools with broad kinase coverage are desirable. A probe that shows outstanding kinase selectivity and allows for the enrichment of up to 133 kinases including many mitogen activated kinase (MAPK) members and JAK kinases has been developed. Furthermore, this probe was applied to establish the selectivity profile of the JAK1/2 inhibitor momelotinib that is currently evaluated in clinical phase 3 studies. These results render this probe a valuable tool for the investigation of JAK and JAK related signaling pathways and the selectivity profiling of kinase inhibitors.