Ontology highlight
ABSTRACT:
SUBMITTER: Puleo DE
PROVIDER: S-EPMC5467198 | biostudies-literature | 2017 Jun
REPOSITORIES: biostudies-literature
Puleo David E DE Kucera Kaury K Hammarén Henrik M HM Ungureanu Daniela D Newton Ana S AS Silvennoinen Olli O Jorgensen William L WL Schlessinger Joseph J
ACS medicinal chemistry letters 20170517 6
Janus kinases (JAKs) regulate hematopoiesis via the cytokine-mediated JAK-STAT signaling pathway. JAKs contain tandem C-terminal pseudokinase (JH2) and tyrosine kinase (JH1) domains. The JAK2 pseudokinase domain adopts a protein kinase fold and, despite its pseudokinase designation, binds ATP with micromolar affinity. Recent evidence shows that displacing ATP from the JAK2 JH2 domain alters the hyperactivation state of the oncogenic JAK2 V617F protein while sparing the wild type JAK2 protein. In ...[more]