Biochemical characterization of CC-509.
- Gregory D. Ferguson (845387)
- Mercedes Delgado (513840)
- Veronique Plantevin-Krenitsky (845388)
- Kristen Jensen-Pergakes (845389)
- R. J. Bates (845390)
- Sanaa Torres (845391)
- Maria Celeridad (845392)
- Heather Brown (19017)
- Kelven Burnett (845393)
- Lisa Nadolny (845394)
- Lida Tehrani (845395)
- Garrick Packard (845396)
- Barbra Pagarigan (613125)
- Jason Haelewyn (845397)
- Trish Nguyen (845398)
- Li Xu (108702)
- Yang Tang (152970)
- Matthew Hickman (83053)
- Frans Baculi (845399)
- Steven Pierce (845400)
- Keiji Miyazawa (412104)
- Pilgrim Jackson (613127)
- Philip Chamberlain (613123)
- Laurie LeBrun (845401)
- Weilin Xie (845402)
- Brydon Bennett (845403)
- Kate Blease (845404)
Publication date
January 2016
DOIAbstract
<p>(A) Chemical structure of CC-509 with IUPAC name of [3-(2H-3,4,5,6-tetrahydropyran-4-ylamino)(1H-indazol-6-yl)][5-(2H-3,4,5,6-tetrahydropyran-4-ylmethyl)(2H-1,2,4-triazolo[1,5-a]pyridin-2-yl)]amine. (B) Representative IC<sub>50</sub> curve (top panel) and K<sub>i</sub> determination (bottom panel) for CC-509 tested against recombinant Syk enzyme. (C) Michaelis-Menten (left panel) and Lineweaver-Burk (right panel) plots for Syk enzyme tested against increasing amounts of substrate and concentrations of CC-509 (shown in nM). (D) Crystallographic diagram of Syk ATP pocket when bound with CC-509. Key residue alanine 451 and hydrogen bonds are shown.</p
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