SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies.

作者: S Hart , K C Goh , V Novotny-Diermayr , C Y Hu , H Hentze

DOI: 10.1038/LEU.2011.148

关键词:

摘要: … downstream of endogenously or ectopically expressed JAK2 … to modulate signaling pathways downstream of JAK2, whether … effects in JAK2 WT - and JAK2 V617F -dependent cells …

参考文章(34)
Bruce D. Cheson, Staging and evaluation of the patient with lymphoma. Hematology-oncology Clinics of North America. ,vol. 22, pp. 825- 837 ,(2008) , 10.1016/J.HOC.2008.07.015
Taghi Manshouri, Alfonso Quintás-Cardama, Roberto H. Nussenzveig, Amos Gaikwad, Zeev Estrov, Josef Prchal, Jorge E. Cortes, Hagop M. Kantarjian, Srdan Verstovsek, The JAK kinase inhibitor CP-690,550 supresses the growth of human polycythemia vera cells carrying the JAK2V617Fmutation Cancer Science. ,vol. 99, pp. 1265- 1273 ,(2008) , 10.1111/J.1349-7006.2008.00817.X
Gerlinde Wernig, Michael G. Kharas, Rachel Okabe, Sandra A. Moore, Dena S. Leeman, Dana E. Cullen, Maricel Gozo, Elizabeth P. McDowell, Ross L. Levine, John Doukas, Chi Ching Mak, Glenn Noronha, Michael Martin, Yon D. Ko, Benjamin H. Lee, Richard M. Soll, Ayalew Tefferi, John D. Hood, D. Gary Gilliland, Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera Cancer Cell. ,vol. 13, pp. 311- 320 ,(2008) , 10.1016/J.CCR.2008.02.009
Ingo Melzner, Marc A. Weniger, Alexandra J. Bucur, Silke Brüderlein, Karola Dorsch, Cornelia Hasel, Frank Leithäuser, Olga Ritz, Martin J.S. Dyer, Thomas F.E. Barth, Peter Möller, Biallelic deletion within 16p13.13 including SOCS-1 in Karpas1106P mediastinal B-cell lymphoma line is associated with delayed degradation of JAK2 protein. International Journal of Cancer. ,vol. 118, pp. 1941- 1944 ,(2006) , 10.1002/IJC.21485
Jeffrey W. Tyner, Thomas G. Bumm, Jutta Deininger, Lisa Wood, Karl J. Aichberger, Marc M. Loriaux, Brian J. Druker, Christopher J. Burns, Emmanuelle Fantino, Michael W. Deininger, CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms Blood. ,vol. 115, pp. 5232- 5240 ,(2010) , 10.1182/BLOOD-2009-05-223727
Carmen Martinez, Emili Montserrat, Mariano Monzo, Alfons Navarro, Tania Diaz, Antonio Martinez, Anna Gaya, Aina Pons, Bernat Gel, Carles Codony, Gerardo Ferrer, Regulation of JAK2 by miR-135a: prognostic impact in classic Hodgkin lymphoma. Blood. ,vol. 114, pp. 2945- 2951 ,(2009) , 10.1182/BLOOD-2009-02-204842
Victoria L. Grandage, Tamara Everington, David C. Linch, Asim Khwaja, Gö6976 is a potent inhibitor of the JAK 2 and FLT3 tyrosine kinases with significant activity in primary acute myeloid leukaemia cells British Journal of Haematology. ,vol. 135, pp. 303- 316 ,(2006) , 10.1111/J.1365-2141.2006.06291.X
Christoph Walz, Brian J. Crowley, Heidi E. Hudon, Jessica L. Gramlich, Donna S. Neuberg, Klaus Podar, James D. Griffin, Martin Sattler, Activated Jak2 with the V617F Point Mutation Promotes G1/S Phase Transition Journal of Biological Chemistry. ,vol. 281, pp. 18177- 18183 ,(2006) , 10.1074/JBC.M600064200
Maria Borrell-Pagès, Federico Rojo, Joan Albanell, Josep Baselga, Joaquín Arribas, TACE is required for the activation of the EGFR by TGF‐α in tumors The EMBO Journal. ,vol. 22, pp. 1114- 1124 ,(2003) , 10.1093/EMBOJ/CDG111
Fabio Zuccotto, Elena Ardini, Elena Casale, Mauro Angiolini, Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation Journal of Medicinal Chemistry. ,vol. 53, pp. 2681- 2694 ,(2010) , 10.1021/JM901443H