Ontology highlight
ABSTRACT:
SUBMITTER: Davis RR
PROVIDER: S-EPMC8327781 | biostudies-literature | 2021 Feb
REPOSITORIES: biostudies-literature
Davis Ryan R RR Li Baoli B Yun Sang Y SY Chan Alice A Nareddy Pradeep P Gunawan Steven S Ayaz Muhammad M Lawrence Harshani R HR Reuther Gary W GW Lawrence Nicholas J NJ Schönbrunn Ernst E
Journal of medicinal chemistry 20210211 4
The discovery that aberrant activity of Janus kinase 2 (JAK2) is a driver of myeloproliferative neoplasms (MPNs) has led to significant efforts to develop small molecule inhibitors for this patient population. Ruxolitinib and fedratinib have been approved for use in MPN patients, while baricitinib, an achiral analogue of ruxolitinib, has been approved for rheumatoid arthritis. However, structural information on the interaction of these therapeutics with JAK2 remains unknown. Here, we describe a ...[more]