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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書誌詳細
出版年:Cancer Discov
主要な著者: 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
フォーマット: Artigo
言語:Inglês
出版事項: 2012
主題:
Article
オンライン･アクセス: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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