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Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.
Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T. Andraos R, et al. Among authors: wyder l. Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3. Cancer Discov. 2012. PMID: 22684457 Free PMC article.
Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.
Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T. Baffert F, et al. Among authors: wyder l. Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29. Mol Cancer Ther. 2010. PMID: 20587663
21 results