Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent

JAK inhibitors are being developed for the treatment of rheumatoid arthritis, psoriasis, myeloproliferative neoplasms and leukemias. Most of these drugs target the ATP-binding pocket and stabilize the active conformation of the JAK kinases. This type-I binding mode leads to an increase in JAK activa...

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Vydáno v:Cancer Discov
Hlavní autoři: Andraos, Rita, Qian, Zhiyan, Bonenfant, Débora, Rubert, Joëlle, Vangrevelinghe, Eric, Scheufler, Clemens, Marque, Fanny, Régnier, Catherine H., De Pover, Alain, Ryckelynck, Hugues, Bhagwat, Neha, Koppikar, Priya, Goel, Aviva, Wyder, Lorenza, Tavares, Gisele, Baffert, Fabienne, Pissot-Soldermann, Carole, Manley, Paul W., Gaul, Christoph, Voshol, Hans, Levine, Ross L., Sellers, William R., Hofmann, Francesco, Radimerski, Thomas
Médium: Artigo
Jazyk:Inglês
Vydáno: 2012
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5022112/
https://ncbi.nlm.nih.gov/pubmed/22684457
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1158/2159-8290.CD-11-0324
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