Your browser doesn't support javascript.
loading
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Alcock, Lisa J; Chang, Yunchao; Jarusiewicz, Jamie A; Actis, Marisa; Nithianantham, Stanley; Mayasundari, Anand; Min, Jaeki; Maxwell, Dylan; Hunt, Jeremy; Smart, Brandon; Yang, Jun J; Nishiguchi, Gisele; Fischer, Marcus; Mullighan, Charles G; Rankovic, Zoran.
Afiliação
  • Alcock LJ; Department of Pathology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Chang Y; Department of Pathology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Jarusiewicz JA; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Actis M; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Nithianantham S; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Mayasundari A; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Min J; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Maxwell D; Department of Pharmacy and Pharmaceutical Sciences, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Hunt J; Department of Pharmacy and Pharmaceutical Sciences, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Smart B; Department of Pharmacy and Pharmaceutical Sciences, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Yang JJ; Department of Pharmacy and Pharmaceutical Sciences, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Nishiguchi G; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Fischer M; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Mullighan CG; Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • Rankovic Z; Department of Pathology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
ACS Med Chem Lett ; 13(3): 475-482, 2022 Mar 10.
Article em En | MEDLINE | ID: mdl-35300081
ABSTRACT
Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ10542 displayed high selectivity over GSPT1 and other members of the JAK family and potency in patient-derived ALL cells containing both JAK2 fusions and CRLF2 rearrangements.
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2022 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2022 Tipo de documento: Article