Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders
Puleo DE, Kucera K, Hammarén H, Ungureanu D, Newton AS, Silvennoinen O, Jorgensen WL, Schlessinger J. Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders. ACS Medicinal Chemistry Letters 2017, 8: 618-621. PMID: 28626521, PMCID: PMC5467198, DOI: 10.1021/acsmedchemlett.7b00153.Peer-Reviewed Original ResearchSmall molecule bindersJAK2 pseudokinase domainKinase foldTyrosine kinase domainNovel pharmacological opportunitiesPseudokinase domainKinase domainJAK-STATJAK2 proteinTop hitsMicromolar affinityPharmacological opportunitiesHyperactivation stateProteinATPJH2JAK2 V617FRecent evidencePseudokinaseMutantsJAKDomainHematopoiesisPathwayStructural approach